015155   Maroliwala J A;Naik B;Desai K R (Chemistry Dep, Faculty of Science, Veer Narmad South Gujarat Univ, Udhna-Magdalla Road, Surat-395 007) : Ecofriendly microwave enhanced synthesis of imidazole derivatives containing coumarin moiety & their antimicrobial activity. Indian J Heterocyclic Chem 2008, 17(4), 363-4.

The synthesis of substituted imidazoles (4a-j) in good yields from the heterocyclization reaction of 3-{[(substituted-1,3-benzothiazol-2-yI) -amino]-acetyl}-2H-chromen-2-ones (3a-j) with KSCN in gl acetic acid under microwave irradiation is being described. Structures of the newly synthesized compounds were elucidated by elemental analysis & spectral data. Some of the new compounds were tested against bacteria (Gram - ve & Gram + ve) & fungi.

1 table, 5 ref

015154   Manna K;Agarwal Y K;Srinivasan K K (Institute of Pharmacy, Nirma Univ of Science and Technology, Ahmedabad) : Synthesis and biological evaluation of new benzofuranyl isoxazoles as antitubercular, antibacterial and antifungal agents. Indian J Heterocyclic Chem 2008, 18(1), 87-8.

Substituted benzofuran chalcones (2a-n) were prepared by the reaction of 2-acetyl benzofuran (1) with different aromatic aldehydes in presence of strong base. Benzofuran chalcones (2a-n) on cyclocondensation with hydroxylamine hydrochloride in presence of sodium acetate, gave various 3-(1-benzofuran-2-yl)-5-phenylisoxazoles (3a-n). The structure of benzofuran isoxazoles 3a-n have been established on the basis of spectral (IR, ¹H NMR, Mass) data. The benzofuran isoxazoles were evaluated for their, antitubercular, antimicrobial and antiinflammatory activities. Some of the compounds have shown promising antitubercular and antibacterial activity.

1 table, 5 ref

015153   Manivel P;Mohana Roopan S;Nawaz Khan F (Chemistry Div, School of Science and Humanities, VIT-Univ, Vellore-632 014, Email: nawaz_f@yahoo.co.in) : Synthesis of o-substituted benzophenones and 1,2-phenylethanones from isocoumarins. Indian J Heterocyclic Chem 2008, 18(1), 21-4.

A series of o-substituted benzophenones and phenylethanones was prepared by efficient method involving 3-substituted isocoumarins and phenylmagnesium bromide and other Grignard reagents. The reaction was completed in presence of dry ether under dry ice conditions in just few minutes with good to excellent yields.

1 table, 5 ref

015152   Mamledesai S N;Katagi M S;Khare P V;Maddi V S;Bhat A R (Pharm. Chemistry Dep, K.L.E. Society's College of Pharmacy, Hubli-580 031) : Synthesis and antimicrobial activity of 4-hydroxy-1-methyl/phenyl-3-substituted quinolin-2-(1H)-ones. Indian J Heterocyclic Chem 2008, 17(4), 381-2.

A series of new 2-quino!one derivatives were synthesized and evaluated for antimicrobial activity against E.coli, S. aureus, C. albicans and A. niger. The new compounds did not show any activity against bacteria however few of the compounds showed good antifungal activity against tested organisms at a concentration of 10-16 μg/ml.

1 table, 2 ref

015151   Mahendran S;Ravi S;Badami S;Suresh B (NO, J.S.S. College of Pharmacy, Rocklands, Ootacamund-643 001) : Isolation of 3,3'-dihydroxy flavonol 7-rhamnoside from Hypericum hookerianum. Indian J Heterocyclic Chem 2008, 18(1), 103-4.

A flavonol, 3,3'-dihydroxy flavonol 7-rhamnoside 1 was isolated from the stem of Hypericum hookerianum for the first time from its ethyl acetate extract.

1 table, 2 ref

015150   Lis A;Nazaruk J;Mielczarek J;Kalemba D (Institute of General Food Chemistry, Technical Univ of Lodz, Stefanowskiego 4/10, 90-924 Lodz, Poland, Email: lisan@vp.pl) : Comparative study of chemical composition of essential oils from different organs of Erigeron annuus (L.) Pers.. J essential Oil Bearing Pl 2008, 11(1), 17-21.

Essential oil from flowers, leaves, stems and roots of Erigeron annuus (L.) Pers. was analyzed by GC, GC-MS and ¹H-NMR spectroscopy. More than 60 compounds were identified. Germacrene D (47.2%) and (Z)-lachnophyllum ester (10.2%) were the main constituents of the flower oil. The leaf oil and stem oil contained mainly germacrene D (55.6% and 44.5% respectively) and β-caryophyllene (9.4% and 13.4%), whereas in the root oil dominated matricaria ester (59.9%) and (Z)-lachnophyllum ester (34.9%).

10 ref

015149   Laxmi Devi A;Nandita Devi T;Biren Singh K; Dhaneshwar Singh M (Chemistry Dep, Manipur Univ, Canchipur, Imphal-795 003) : Synthesis and stereochemistry of N⁴-aryl-1-1,2,4-triazoles.. Indian J Heterocyclic Chem 2008, 18(1), 41-4.

N⁴-Aryl-1,2,4-triazoles have been synthesized. These triazoles carry bulky substituents at 3,5-positions of the triazole ring and 2',6'-positions of the N-aryl ring. Restricted rotation and non-planar conformation about the N-aryl (Nsp²-Csp²) bond have been observed.

10 ref

015148   Kubmarawa D;Ogunwande I A (Chemistry Dep, Federal Univ of Technology, P.M.B. 2076, Yola, Adamawa State, Nigeria, Email: dkubmarawa@yahoo.com) : Composition of the leaves essential oil of Calotropis procera (R.Br.) from Nigeria. J essential Oil Bearing Pl 2008, 11(1), 75-8.

Leaf essential oil of Calotropis procera (R.Br.) was analysed by GC and GC-MS. The leaf oil contained phytol (33.6%), myristic acid (31.2 %) and myristicin (19.9%) as major constituents.

1 table, 13 ref

015147   Kini S G;Bhat A R;Bhat R;Narayanaswamy N (Pharmaceutical Chemistry Dep, Manipal College of Pharmaceutical Sciences, Manipal-576 104) : Synthesis and antimicrobial activity of new 3,5-disubstituted isoxazoles. Indian J Heterocyclic Chem 2008, 17(4), 319-22.

New 3,5 disubstituted isoxazoles were prepared by the action of hydroxylamine hydrochloride and sodium acetate on 3-{3-[3-(trifluoromethyl) phenoxy/phenoxy]-4-substituted phenyl/phenyl}-1-(4-substitutedphenyl)-2-propene-1-ones (chalcones) (II). The structures of the synthesized compounds were settled on the basis of spectral data. The antibacterial, antitubercular and antifungal activities of all compounds have been evaluated. Compounds carrying halogen on a-ring showed strong antimicrobial activity. However the titled compounds exhibited moderate antifungal activity. Some compounds exhibited significant activity towards a strain of Mycobacterium tuberculosis H₃₇Rv.

1 tablel, 10 ref

015146   Khandelwal S P;Amnerkar N D;Khedekar P B; Bhusari K P (NO, Sharad Pawar College of Pharmacy, Wanadongri, Hinga Road, Nagpur-441 110) : Synthesis and biological evaluation of some thio substituted 1,4-dihydropyrimidine-5-carboxylates. Indian J Heterocyclic Chem 2008, 18(1), 77-80.

A series of pyrimidine-5-carboxylates (VIa-o) were synthesized by condensing methyl-6-methyl-4-(substituted phenyl)-2-thio-1,2,3,4-tetrahydro-pyrimidine-5-carboxylates (IVa-e) with 2-chloro-N-(substituted phenyl) acetamides (Va-e) in presence of alcoholic potassium hydroxide. The structures of all the newly synthesized compounds were characterized by elemental analysis and spectroscopic data such as UV, IR, ¹H NMR. Further, they were screened for antimicrobial and analgesic activity.

2 tables, 8 ref

015145   Kamat V D;Mandhare P N (P.G. Dep of Chemistry, Mahatma Phule Arts, Science and Commerce, College, Panvel, Navi Mumbai-410 206) : Synthesis of 5-(4-substituted phenyl)-2-phenyl oxazoles. Indian J Heterocyclic Chem 2008, 17(4), 369-70.

Nitro, sulphonyl, chloro-sulphonyl and bromo derivatives of 5-(4-substituted phenyl)-2-phenyl oxazoles were prepared by treating 2,5-diphenyl oxazole with H₂SO₄/HNO₃ H₂SO₄/20% oleum, chloro-sulphonic acid and liq. bromine respectively.

2 ref

015144   Kalluraya B;Rao J N;Sujith K V (Studies in Chemistry Dep, Mangalore Univ, Mangalagangothri-574 199) : Microwave assisted one-pot synthesis of some 2,5-disubstituted 1,3,4-oxadiazoles. Indian J Heterocyclic Chem 2008, 17(4), 359-62.

The series of 2,5-disubstituted 1,3,4-oxadiazoles 4 were synthesized by the reaction of 3-pyridyl or 2-methyl-5-nitro-1-imidazomethyl hydrazide and aromatic aldehydes in the presence of eerie ammonium nitrate in dichloromethane as well as by microwave irriadiation in ethanol.

1 table, 8 ref

015143   Kakade G K;Madje B R;Pokalwar R U;Ware M N; Shingare M S (Chemistry Dep, Dr. Babasaheb Ambedkar Marathwada Univ, Aurangabad-431 004) : DBU catalyzed knoevenagel condensation under ultrasonic irradiation. Indian J Heterocyclic Chem 2008, 17(4), 379-80.

The condensation reaction of 2-chloroquinoline-3-carbaldehyde with ethyl cyanoacetate was carried out under ultrasonic irradiation catalyzed by 1,8-diazabicyclo-undec-7-ene (DBU) at room temp under solvent free condition to afford ethyl 3-(2-chloro substituted quinolin-3-yl)-2-cyanoacrylates 3a-h.

1 table, 2 ref

015142   Joshi S D;Vagdevi H M;Vaidya V P;Gadaginamath G S;Purohit S S (P.G. Studies and Research in Chemistry Dep, School of Chemical Science, Kuvempu Univ, Jnana Sahyadri, Shankaraghatta-577 451) : Synthesis, antibacterial and antitubercular activities of some new 3-substituted phenyl-5-(4-pyrrol-1-ylphenyl)-4H-1,2,4-triazoles. Indian J Heterocyclic Chem 2008, 17(4), 367-8.

A new series of triazole derivatives were synthesized and the structures of these compounds were confirmed by IR, ¹H NMR and CHN analysis. The title compounds were screened for antibacterial and antitubercular activities.

1 table, 11 ref

015141   Joshi A;Bapna A;Talesara G L (Synthetic Organic Chemistry Laboratory, Chemistry Dep, M.L. Sukhadia Univ, Udaipur-313 001) : Synthesis and antimicrobial screening of some {5-arylidene-3-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl-oxy) ethyl]-4-oxo-1,3-thiazolidin-2-ylidene} nicotinohydrazides. Indian J Heterocyclic Chem 2008, 18(1), 45-8.

Some {5-arylidene-3-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl-oxy) ethyl]-4-oxo-1,3-thiazolidin-2-ylidene} nicotinohydrazides (6a-d) have been synthesized by the condensation of 5-arylidene-2-nicotinoylhydrazido-1,3-thiazolidin-4-ones (5a-d) with ω-bromoethoxyphthalimide (III) in presence of catalytic amount of pyiridine. Treatment of substituted araldehydes (4a-d) with 2-nicotinoylhydrazido-1,3-thiazolidin-4-one (3) gave corresponding arylidene derivatives (5a-d). Nicotinoylhydrazine carbothioamide (2) when refluxed with chloroacetic acid in the presence of anhyd sodium acetate furnished compound (3) which in turn was obtained by the addition of NH₄SCN to nicotinic acid hydrazide (I) in acidic media. The structures of newly synthesized compounds were established on the basis of elemental analysis, IR, ¹H NMR and mass spectral data. Final compounds were screened for their antimicrobial activities against E. coli, B. subtilis, P. aeruginosa, S. typhi and C. albicans, A. fumigatus.

6 ref

015140   Jayanthi P;Lalitha P;Sripathi S K (Chemistry Dep, Avinashilinagam University for Women, Coimbatore-641 043, Email: goldenlalitha@gmail.com) : Use of lawesson's reagent in the facile synthesis of few thiones. Asian J expl Sci 2009, 23(1), 123-6.

A simple and facile method for the synthesis of thiones has been developed. Lawesson's Reagent ((,4-bis (4-methoxy phenyl)-l,3-dithia-2, 4-diphosphethane-2,4-disulfide),a versatile and effective thionation reagent has been used for the conversion of the carbonyl moiety in quinolones to the thiocarbonyl moiety. The time of synthesis was less; work was simple, since the products are obtained in a one- pot synthesis. A suitable mechanism for the formation of has been proposed.

3 tables, 10 ref

015139   Jamode V S;Chandak H S;Bhagat P R (Chemistry Dep, G.S. Science, Arts & Commerce College, Khamgaon-444 312) : Synthesis and antimicrobial activities of some N-[3-(2,3-dibromo-3-arylpropanoyl) phenyl]-benzenesulfonamides and their derived pyrazoles. Indian J Heterocyclic Chem 2008, 18(1), 37-40.

A series of N-[3-(2,3-dibromo-3-aryl-propanoyl) phenyl]-benzenesulfonamides (IIa-e) have been synthesized and refluxed with isonicotinoic acid hydrazide and semicarbazide in pyridine medium to afford N-{3-[5-aryl-1-(4-pyridoyl)-pyrazol-3-yl]-phenyl}-benzenesulfonamides (Illa-e) & 3-(3-benzenesulfonyl-amino-phenyl)-5-aryl-pyrazole-1-carboxylic acid amides (IVa-e) respectively. The synthesized compounds have been assayed for antibacterial activities against Staphylococcus aureus (gram +ve), Escherichia coli, Proteus mirabilis & Pseudomonas aeruginosa (gram-ve) using paper disc diffusion method.

1 table, 3 ref

015138   Jag Mohan;Rathee A (Chemistry Dep, M.D. Univ, Rohtak-124 001) : Bridgehead nitrogen spiroheterocyclic systems : synthesis and antimicrobial activity of spiro-[3H-5-bromoindole-3,2'-thiazolidine]-2-[1H], 4'-(5'H)-diones and CIS-3',3a-dihydrospiro [3H, 5-bromoindole-3,5'-pyrazolo [3',4':4,5]-thiazol-2-(1H)-ones. Indian J Heterocyclic Chem 2008, 17(4), 327-30.

Condensation of isatin-3-imines 1 with thioglycollic acid gave 3'-arylspiro [3H, 5-bromoindole-3,2'-thiazolidine]-2-(1H), 4'-(5'H)-dione 2 which on condensation with aldehydes furnished 5'-arylidene derivatives 3. Treatment of 3 with 2,4-dinitrophenylhydrazine gave 4. The structures of 2,3 & 4 have been supported by IR, ¹H NMR spectral data. The antibacterial and antifungal activities of some of the compounds have also been evaluated.

9 ref

015137   Jadhav J S;Chatpalliwar V A;Khadse S C;Patil R R (Pharmaceutical Chemistry Dep, R.C. Patel College of Pharmacy, Karvand Naka Shirpur, Dist. Dhule-425 405) : Synthesis and screening of some new 2-(3H)-benzoxazolone derivatives for analgesic, antiinflammatory and skeletal muscle relaxant activity. Indian J Heterocyclic Chem 2008, 17(4), 343-6.

Some 2-(3H)-benzoxazolone derivatives (C₁-C₄) were synthesized by coupling chlorzoxazone with substituted benzimidazoles (I-Ic) for synergistic action. Synthesized compounds were characterized by spectral analysis (UV, IR and NMR & Mass) and subjected to pharmacological screening for antiinflammatory, analgesic and skeletal muscle relaxant activities.

7 ref

015136   Hossain A M S;Nazimuddin M;Dutta S;Begum J (Chemistry Dep, Chittagong Univ, Chittagong-4331, Bangladesh, Email: monsur_12@yahoo.com) : Antimicrobial activities of tetradentate bis [<. Bull pure appl Sci-Sect C 2008, 27(2), 87-94.

Six tetradentate bis (⁴N-substituted thiosemicarbazones) and their nickel (II) and copper(II) complexes were screened for their in vitro antimicrobial activities against six phytopathogenic fungi and six human pathogenic bacteria including three gram positive and three gram negative bacteria. All the ⁴N-substituted bis (thiosemicarbazones) and their metal complexes were found to exhibit promising antifungal activities against the fungal pathogens. The highest inhibition was recorded for Macrophomina phaseolina followed by Botryodiplodia theobromae. However, all the ligands and their copper (II) complexes showed moderate antibacterial activities against the test bacterial pathogens. Coordination of the ligands to nickel (II) ions did not enhance growth inhibition of any of the test bacteria.

2 tables, 28 ref

015135   Havaldar F H;Patil A R (Nadkarny-Sacasa Research Laboratory, Chemistry Dep, St. Xavier's College, Mumbai-400 001) : Synthesis of new triazolo-thiadiazoles and their antimicrobial activity. Indian J Heterocyclic Chem 2008, 18(1), 61-4.

A series of 6-(substituted phenyl)-3-(3-methyl-5-nitro-imidazol-1 -yl methyl)-5,6-dihydro-[1,2,4] triazolo [4,3-b] [1,3,4] thiadiazoles (5a-e) have been synthesized by cyclization of 4-amino-5-(2-methyl-5-nitro-imidazol-1-yl methyl)-4H-[1,2,4] triazol-3-thiol (4) with various aromatic aldehydes. The structures of the newly synthesized compounds have been confirmed by IR, ¹H NMR and mass spectral data. The compounds have been screened for their biological activity.

13 ref

015134   Havaldar F H;Bhise S S;Burudkar S (Nadkarny-Sacasa Research Laboratory, Chemistry Dep, St. Xavier's College, Mumbai-400 001) : Convenient synthesis and biological activity of 2-azetidinones and 4-thiazolidinones. Indian J Heterocyclic Chem 2008, 18(1), 57-60.

4-Hydroxy coumarin was reacted with ethyl chloroformate in the presence of anhyd potassium carbonate to yield ethyl 2-oxo-2H-chromen-4-yl carboxylate (1) which gave a hydrazide, 2-oxo-2H-chromen-4-yl hydrazine carboxylate (2) with hydrazine hydrate. The compound (2) on condensation with various aromatic aldehydes in gl acetic acid gave, 2-oxo-2H-chromen-4-yl-2-(substituted benzylidene) hydrazine carboxylates (3a-f) which on further treatment with chloroacetyl chloride and thioglycollic acid afforded 2-oxo-2H-chromen-4-yl-3-chloro-2-oxo-4-(substituted phenyl)-azetidin-1-yl carbamates (4a-f) and 2-oxo-2H-chromen-4-yl-4-oxo-2-(substituted phenyl)-1,3-thiazolidin-3-yl carbamates (5a-f) respectively. The structures of all the newly synthesized compounds have been established by analytical and spectral methods. Their purity has been ascertained by chromatographic resolution. Some of the compounds showed significant antibacterial activity.

1 table, 2 ref

015133   Goudgaon N M;Upendar Reddy C H;Roopa S (Studies and Research in Chemistry Dep, Gulbarga Univ, Gulbarga-585 106) : Synthesis of novel 5-phenylthio-2,4-disubstituted pyrimidine analogs. Indian J Heterocyclic Chem 2008, 18(1), 25-8.

5-Phenylthio-2,4-disubstituted pyrimidines were prepared in three steps starting from 5-chlorouracil. Reaction of 5-chlorouracil with thiophenol under basic condition furnished the desired 5-phenylthiouracil, which on chlorination using excess POCl₃ yielded the synthon 5-phenylthio-2,4-dichloropyrimidine. Aromatic nucleophilic substitution reaction of 5-phenylthio-2,4-dichloropyrimidine with various oxygen nucleophiles like sodium phenoxides and nitrogen nucleophiles like aliphatic primary amines, substituted aromatic primary amines and substituted heterocyclic primary amines furnished the target compounds, 5-phenylthio-2,4-disubstituted pyrimidines in 55-97% yield.

1 table, 4 ref

015132   Goudgaon N M;Upendar Reddy C H (Studies and Research in Chemistry Dep, Gulbarga Univ, Gulbarga-585 106) : Synthesis of novel 1,5-disubstituted uracils. Indian J Heterocyclic Chem 2008, 18(1), 97-8.

1,5-Disubstituted uracils 2a-p were prepared efficiently in a single step, via the reaction of 5-substituted uracils 1a-d with diaryliodonium salts as strong electrophiles under anhyd condition in presence of sodium hydride and dry DMF in 50-75% yield.

1 table, 4 ref

015131   Ghosh S;Malik S;Jain B;Ganesh N (NO, , 33/2B, Saket Nagar, Hopal-462 024, Email: suparnabpl@yahoo.co.in) : Synthesis, characterization and biological studies of Zn(II) complex of schiff base derived from 5-acetazolamido-1,3,4 - thiadiazole-2-sulphonamide, a diuretic drug. Asian J expl Sci 2009, 23(1), 189-92.

Five-acetazolamido-l,3,4-thiadiazole-2-sulphonamide, trade name acetazolamide, is a diuretic drug (Diuretic drugs increase the output of urine through kidneys). In the present communication, the metal complex of Zn(II) with schiff base derived from salicyladehyde and 5-acetazolamide -1,3,4 - thiadiazole-2-sulphonamide have been synthesized keeping in view that some metal complexes are found to be more potent than their parent drugs. These complexes were characterized on the basis of elemental analysis, conductivity, IR and ¹H NMR spectral studies. The analytical data reflects the metal to ligand stoichiometry to be 1: 2. The ratio of complex formation with the above metal was further confirmed conductometrically using Job's method of continuous variation. The conductivity data of the complexes also suggests their non-electrolytic nature. The stability constants and free energy change for the complexes have been calculated. The diuretic activity of these complexes was checked on albino rats and the results have been found to be very encouraging.

3 tables, 9 ref

015130   Fazal Mohamed M I;Seeni Mubarak M (Postgraduate and Research Dep of Chemistry, Jamal Mohamed College (Autonomous), Tiruchirappalli-620 020) : Synthesis of 2,4-diphenyl-3-azabicyclo [3,3,1] nonan-9-ones. Indian J Heterocyclic Chem 2008, 18(1), 91-2.

The compound 2,4-diphenyl-3-azabicyclo-[3,3-1] nonan-9-one (1) has been synthesized on the basis of Mannich type condensation using ammonium formate as the newly identified cyclizing agent in this study. Semicarbazone (2), thiosemicarbazone (3) and spiro-tetrazine (4) derivatives of 1 have also been prepared. Compounds (1-4) were characterized by IR, ¹H NMR, ¹³C NMR, Mass and elemental analysis. The above compounds have been screened for antimicrobial and antifungal activity. The semicarbazone, thiosemicarbazone and spiro-tetrazine derivatives of 1 are found to be active against gram positive organisms Staphylococcus aureus and Streptococcus fecalis, the gram negative organisms E.coli and Pseudomonas aeruginosa, Further, all the derivatives are active against fungi Candida albicans.

2 ref

015129   Dixit R;Dixit Y;Gautam N;Gautam D C (Chemistry Dep, Rajasthan Univ, Jaipur-302 004, Email: rahuldixit_uour.yahoo.co.in) : Synthesis and antimicrobial activities of novel 4H-1,4-benzothiazines and their sulfones. Indian J Heterocyclic Chem 2008, 17(4), 323-6.

An elegant one step synthesis of substituted 4H-1,4-benzothiazines 4 has been achieved by the condensation of substituted 2-aminobenzenethiols 1 with β-diketones 2 in dimethyl sulfoxide. Compounds 4 on refluxing with 30% hydrogen peroxide in gl acetic acid undergo oxidation and afford their sulfones 5. All the synthesized compound have been characterized by IR, ¹H NMR, Mass spectra and elemental analysis and screened for their antibacterial and antifungal activities.

1 table, 13 ref

015128   Diwakar S D;Shingare M S;Gill C H (Chemistry Dep, Dr. Babasaheb Ambedkar Marathwada Univ, Aurangabad-431 004) : DI-fluorobenzimidazole and 1,2,3-triazole incorporated chromones: synthesis and antimicrobial activity. Indian J Heterocyclic Chem 2008, 18(1), 49-52.

Chromones 9a-h containing benzimidazole and triazole moiety were synthesized by condensation of active methylene sandwiched in between 4-nitrophenyl and benzimidazole with 3-formyl chromones followed by alkylation with triazolyl bromide 6. The synthesized compounds were evaluated for antibacterial activities.

1 table, 10 ref

015127   Dinakaran V;Unnissa H;Kalishwari E (Pharmaceutical Chemistry Dep, MCOPS, Manipal-576 104) : Synthesis and antibacterial activity of some 2,3-disubstituted quinazolin-4(3H) ones. Indian J Heterocyclic Chem 2008, 17(4), 347-50.

Some new 2,3-disubstituted quinazolin-4-(3h)-ones have been synthesized by the condensation of respective 2-substituted 1,3-benzoxazin-4-ones (4a-b) with different primary amines in equimolar conc. The structures of these compounds have been established on the basis of their elemental, analytical and spectral data. These compounds were tested for invitro antibacterial activity against Staphylococcus aureus (ATCC 9144), Staphylococcus epidermidis (ATCC 155), Micrococcus luteus (ATCC 8341), Ktebsiella pneumonias (ATCC 29665) and Escherichia coli(ATCC 25922).

1 table, 7 ref

015126   Diaz Maroto M C;Castillo N;Castro-Vazquez L; Torres C D;Perez Coello M S (NO, IRICA (Instituto Regional de Investigacion Cientifica Aplicada), s/n, 13071 Ciudad Real, Spain, Email: MariaConsuelo.Diaz@ulem.es) : Authenticity evaluation of different mints based on their volatile composition and olfactory profile. J essential Oil Bearing Pl 2008, 11(1), 1-16.

Evaluated the authenticity of different mints, commercialised by the names of peppermint, spearmint or only mint, their volatile oil extracts were obtained by simultaneous distillation-extraction and analysed by gas chromatography-mass spectrometry. In peppermint leaves trans-p-menthone and L-(-)-menthol were the major components, followed by trans-menthyl acetate, 1,8-cineole and limonene, trans-sabinene hydrate, and cis-p-menthone. (R)-(-)-Carvone was the major component in the spearmint oil extracts, together with 1,8-cineole and limonene. A screening for ranking odorants present in these aromatic plants was realised by gas chromatography-olfactometry. Among the compounds with high odour intensities, 1,8-cineole, trans-p-menthone, neomenthol and L-(-)-menthol had the characteristic minty notes of peppermint. However, only L-(-)-menthol presented the cooling sensation of this aromatic plant. (R)-(-)-Carvone, with sweet and spearmint odours, was identified as the key compound contributing to the aroma of spearmint oil extracts. GC-O technique, based on the measurement of odour intensities using simple rating scales, can be a useful screening tool for ranking the odorants of very complex samples such as aromatic plants, and together with GC-MS permit the detection of any type of mixture or adulteration of commercial mints.

4 tables, 28 ref

015125   Davoodnia A;Rahimizadeh M;Atashi S (Chemistry Dep, School of Sciences, Islamic Azad Univ, Mashhad Branch, Mashhad-91735-413, Iran, Email: adavoodnia@yahoo.com) : Synthesis of new functionalized fused heterocyclic compounds derived from isoxazole : isoxazolo [4,5-d] pyrimidin-4-(5H)-ones, isoxazolo [5,4-d] [1,3] oxazin-4-one and isoxazolo [5,4-d] [1,3] thiazin-4-one. Indian J Heterocyclic Chem 2008, 18(1), 89-90.

New functionalized derivatives isoxazolo [5,4-d] pyrimidin-4(5H)-ones (3), isoxazolo [5,4-d] [1,3] oxazin-4-one (4) and isoxazolo [5,4-d] [1,3] thiazin-4-one (5) have been prepared via cyclocondensation of ethyl 5-amino-3-methylisoxazole-4-carboxylate with aryl nitriles, sodium cyanate and potassium thiocyanate respectively.

6 ref

015124   Davoodnia A;Bakavoli M;Elmi-Mehr M (Chemisty Dep, School of Sciences, Islamic Azad Univ, Mashhad Branch, Mashhad-91735-413, Iran, Email: adavoodnia@yahoo.com) : Synthesis of new isoxazolo [5,4-d] [1,3] oxazine derivatives. Indian J Heterocyclic Chem 2008, 17(4), 371-2.

New derivatives of isoxazolo [5,4-d] [1,3] oxazines have been prepared via heterocyclization of 5-amino-3-methylisoxazole-4-carboxylic acid with triethylorthoesters.

9 ref

015123   Das B;Thirupathi P;Rathod A K (Organic Chemistry Div-I, Indian Institute of Chemical Technology, Hyderabad-500 007) : Sulfated zirconia as an efficient recyclable heterogeneous catalyst for selective aminolysis of epoxides and N-tosyl aziridines under solvent-free condition. Indian J Heterocyclic Chem 2008, 17(4), 339-42.

Sulfated zirconia has been found to be an efficient catalyst for selective ring-opening of epoxides and N-tosyl aziridines with amines under solvent-free conditions to form the corresponding 2-amino alcohols and 1,2-diamines respectively in excellent yields. The catalyst can be recovered and recycled.

2 tables, 6 ref

015122   Dabholkar V V;Ansari F M (Organic Research Laboratory, Chemistry Dep, K.C. College, Churchgate, Mumbai-400 020, Email: vijudabhholkar@hotmail.com) : Ultrasound mediated synthesis of biologically active spiro compounds. Indian J Heterocyclic Chem 2008, 17(4), 335-8.

New spiro heterocyclic system namely 3,9-dioxo-4,8-di-(3'-aryl) carbamid-13,13-dimethyl-1,11-dithia-4,8-diaza-bispiro [4.1.4.3] tetradecanes (4) have been synthesized from semicarbazone of 5,5-dimethyl cyclohexan-1,3-dione (3) and thiogylcollic acid. The compounds (4) on further treatment with cone H₂SO₄ cyclized to form bispiro-5,5-dimethyl [cyclohexane-1,2':3.2"-di-(1,3-thiazolo-4-en) [3,4-b]-2-arylamino)-1,3,4-oxadiazoles] (5). The structures of synthesized compounds were confirmed by IR, ¹H, ¹³C NMR and Mass spectral data.

1 table, 5 ref

015121   Cole R A;Haber W A;Setzer W N (Chemistry Dep, Alabama in Huntsville, Huntsville, AL 35899, USA, Email: wsetzer@chemistry.uah.edu) : Leaf oil composition of Myrcia splendens from Monteverde, Costa rica. J essential Oil Bearing Pl 2008, 11(1), 41-4.

Leaf essential oil of Myrcia splendens Standl. (Myrtaceae), from Costa Rica, was isolated by hydrodistillation and analyzed by GC-MS. A total of 26 compounds were identified in the leaf oil accounting for 96.9% of the total composition. The most abundant components of the leaf oil of M. splendens were germacrene D (35.9%), valerianol (16.3%) trans-2-hexenal (9.5%), epi-α-cadinol (6.8%), and 5-cadinene (5.8%).

1 table, 8 ref

015120   Bhosale S S;Shaikh M S;Coutinho E C;Saran A (Pharmaceutical Chemistry Dep, Bombay College of Pharmacy, Kalina, Santacruz (E), Mumai-400 098, Email: evans@bcpindia.org) : Application of molecular electrostatic potentials in drug design. Proc Indian Natn Sci Acad 2007, 73(2), 91-110.

Molecular electrostatic potential (MEP) is a representation of the electrostatic interaction energy between a molecule and a unit positive test charge placed at that point, with the assumption that the molecule is not polarized by the test charge. It is an extensively used parameter to study a variety of chemical and physical properties and is also valuable for exploring the structure and reactivity of molecules. It has now been accepted that complementary MEP pattern is responsible for the molecular recognition process of a ligand with its receptor to show a particular pharmacological action. In this review, we present the theoretical aspects of MEP and various parameters derived from MEP along with its application in the field of QSAR, the design of transition state analogs, the prediction of toxicity, and in the design of biomolecules with specific molecular attributes.

^iia7 illus, 93 ref

015119   Bhanushali M D;Pujari R W;Bhat A R (Pharmaceutical Chemistry Dep, K.L.E.S.'s, College of Pharmacy, Belgaum-590 010) : Synthesis and antimicrobial activity of some substituted phenothiazines. Indian J Heterocyclic Chem 2008, 18(1), 99-100.

Reaction of phenothiazine with p-amino benzoic acid and benzaldehyde in ethanol furnishes 10 (α-4-carboxyphenyl-aminobenzyl) phenothiazine PB₁ which was condensed with various substituted anilines to give P₁-P₃. 10-(α-4-Carboxyphenyl-aminobenzyl) phenothiazine was esterified followed by condensing with substituted anilines and INH to give P₄-P₆. All the compounds were evaluated for antibacterial and antifungal activities. Most of the compounds have shown significant antibacterial and antifungal activity when compared with the standard drug.

1 table, 4 ref

015118   Basawaraj R;Goled S N;Kalaskar G;Sangapure S S (Post-Graduate Centre, Pharmaceutical Chemistry Dep, Karnataka College of Pharmacy, Bidar-585 403) : Reaction products of 2-substituted-4-chlorobenzofuro [3,2-d] pyrimidines and their antimicrobial activities. Indian J Heterocyclic Chem 2008, 18(1), 1-4.

The nucleophilic displacement reaction of 2-substituted-4-chlorobenzofuran [3,2-d] pyrimidines 4-5 with nucleophiles such as sodium methoxide, sodiumethoxide and thiourea furnished 2-substituted-4-met.hoxy/ethoxy benzofuro [3,2-d] pyrimidines 6-9 and 2-substituted-3,4-dihydro-4-thiobenzofuro [3,2-d] pyrimidines 10-11 respectively. All the synthesized compounds were characterized on the basis of analytical and spectral data. These compounds were screened for their antimicrobial activities.

1 table, 8 ref

015117   Basavaraja K M;Somasekhar B;Appalaraju S (Industrial Chemistry Dep, Gulbarga Univ, Post Graduate Centre, Hospet Road, Bellary(Cant)-583 104) : Synthesis and biological activity of some 2-[3-substituted-2-thione-1,3,4-thiadiazole-5-YL] aminobenzothiazoles. Indian J Heterocyclic Chem 2008, 18(1), 69-72.

Chloro/fluoro substituted-2-aminobenzothiazole (1) was condensed with carbon disulfide and hydrazine hydrate to get (II) which on cyclisation with carbon disulfide in presence of TEA produced (III). Treatment of (III) with formaldehyde and substituted amines gave 2-[3-substituted-2-thione-1,3,4-thiadiazole-5-yl] amino benzothiazoles (IV). All the newly synthesized compounds have been characterized by spectral and elemental analysis. These compounds were screened for antimicrobial, antiinflammatory and analgesic activity; some of them exhibited appreciable activity.

2 tables, 12 ref

015116   Basavaraja B M;Vagdevi H M;Srikrishna L P; Shubha B S;Vaidya V P (Industrial Chemistry Dep, Kuvempu Univ, Shankaraghatta-577 451) : Synthesis and antimicrobial activity of 1,3,4-oxadiazole incorporated benzoxazoles. Indian J Heterocyclic Chem 2008, 18(1), 5-8.

The compounds 5-[(1,3-benzoxazol-2-yl-thio) methyl]-1,3,4-oxadiazole-2-thiols 3a-b have been synthesized from 2-[(5-methyl-1,3-benzoxazol-2-yl) thio] aceto hydrazides 2a-b by refluxing with carbon disulphide in presence of alcoholic potassium hydroxide. The title compounds 5-[(1,3-benzoxazol-2-yl-thio) methyl]-3-{[(4-substitutedphenyl) amino] methyl}-1,3,4-oxadiazolidine-2-thiones 4a-p were prepared from 5-[(1,3-benzoxazol-2-yl-thio) methyl]-4,5-dihydro-1,3,4-oxadiazole-2-thiones 3a-b by stirring with formaldehyde and appropriate aromatic amines in ethanol. All the synthesized compounds were characterized by spectral data and evaluated for antimirobial activity by cup plate method. Many compounds were found to exhibit significant antibacterial and antifungal activities.

1 table, 8 ref

015115   Basavaiah K;Anil Kumar U R (Chemistry Dep, University of Mysore, Manasagangotri, Mysore-570 006, Email: basavaiahk@yahoo.co.in) : Development and validation of a new HPLC analytical method for the determination of zidovudine in pharmaceuticals. Proc Indian Natn Sci Acad 2007, 73(2), 51-4.

A new analytical method is developed and appropriately validated by means of a high resolution liquid chromatography (HPLC) of reverse phase to quantify zidovudine in pharmaceutical preparations. The HPLC determination was performed on Ii reversed phase column (Hypersil C₁₈ 5,μm; 250x4.6 mm i.d) using a mobile. phase (1 mL min^-1 ) consisting of water: acetonitrile-85:15 (v/v) with UV-detection at 265 nm. A rectilinear relationship between mean peak area and concentration of ZDV was observed in the range 50-750 ,ug mL^{-1 with a detection limit of 6.0 ,μg mL-1 and a quantitation limit of 20.0,μg mL-1. Intra-day and Inter-day precision, and accuracy of the methods have been established according to the current ICH guideiines. The results were statistically compared with those of the reference method by applying Student's t-test and F-test. Accuracy, evaluated by means of the spike recovery method was in the range 97.7-103.2%, with precision (RSD) better than 2%.}

3 illus, 3 tables, 19 ref

015114   Ashok Kumar B S;Lakshman K;Jayaveera K N; Vamshi Krishna N;Manjunath M;Suresh M V (Pharmacognosy Dep, Sri K.V. College of Pharmacy, Chickballapur, Karnataka, Email: ashok4vani@gmail.com) : Estimation of rutin and quercetin in Amaranthus viridis Linn by HPLC. Asian J expl Sci 2009, 23(1), 51-4.

Amaranthus viridis, is traditionally used for treatment of constipation, inflammation, eczema, bronchitis, anemia, leprosy. Flavonoids are a group of polyphenolic compounds, which are widely distributed through out the plant kingdom. Flavonoids like Rutin and quercetin possess many biochemical effects like inhibition of enzymes, regulatory role on different hormones and pharmacological activities like antimicrobial, antioxidant, and anticancer, antihepatotoxic, protection of cardio vascular system. An HPLC method was developed for the estimation of rutin and quercetin from methanol herbal extract of Amaranthus viridis.

13 ref

015113   Arun Kumar;Seth R (Dairy Chemistry Div, National Dairy Research Institute, Karnal-132 001) : Chemical quality of spray dried skim milk powder. Indian J Dairy Sci 2008, 61(1), 27-30.

Skim milk powder (SMP) of twenty-eight brands manufactured in 7 states was analyzed for its chemical quality. The overall chemical composition of SMP from different states showed wide variations, clearly indicating the variation in initial milk quality, the processing and storage conditions. Chemical quality revealed that acidity of SMP samples from Delhi and Uttar Pradesh was significantly lower, i.e., 1.25±0.06 percent and 1.27±0.07 percent, respectively. Similarly, the lactate content in SMP samples collected from Delhi and Haryana was higher, i.e. 367.5±73.30 and 261.25±59.94 mg/100 gm SMP, respectively. Two brands out of four brands of Delhi and Haryana were found positive for alkaline neutralizers.

3 tables, 6 ref

015112   Anand M;Dhanasekaran V;Arulprakash G; Guhanathan S (Chemistry Div, School of Science and Humanities, VIT Univ, Vellore-632 014, Email: sai_gugan@yahoo.com) : Synthesis of 2-allylbenzo [d] isoxazol-3-(2H)-ones. Indian J Heterocyclic Chem 2008, 18(1), 85-6.

The reaction of methyl salicylate hydroxylamine hydrochlon'de provided the respective N,2-dihydroxybenzamide 1, which was further treated with thionyl chloride in tetrahydrofuran and triethylamine in 1,4 dioxan to give benzo [d] isoxazol-3-(2H) one 2. 2 was further treated with various allyl bromides to give the title compounds 2-allylbenzo [d] isoxazol-3 (2H)-ones 3.

1 table, 5 ref

014092   Vidyasagar Babu S;Hussain Reddy K;Lingappa Y (Chemistry Dep, Sri Krishnadevaraya Univ, Anantapur-515 003, Email: khussainreddy@yahoo.co.in) : Spectrophotometric determination of cobalt in biological samples using 2-acetylpyridine semicarbazone. J Indian Chem Soc 2009, 86(3), 312-15.

Analytical application of 2-acetylpyridine thiosemicarbazone (APT) and 2-acetylpyridine semicarbazone is described for the direct non-extractive spectrophotoraetric determination of cobalt. The reagents react with cobalt in acidic medium (pH 6.0, sodium acetate-acetic acid buffer) to form orange yellow colored 1 : 2 (M : L) complexes. The colour reactions are instantaneous and absorbance values remain constant for over 24 h. The molar absorptivity and Sandell's sensitivity of APT and APS methods are found to be 1.25 x 10⁴ and 1.45 x 10⁴ L mol^-1 cm¹ and 0.0047 and 0.004 fig cm^-2 of Co^II respectively. The systems obey Beer's law in the range of 0.236-2.357 μg/ml of Co^II. Since APS method is more sensitive it was applied for the determination of cobalt in biological samples.

^ssc2 tables, 9 ref

014091   Verma H S;Vinod Kumar (Chemistry Dep, J.V. College, Baraut-250 611, Email: vinodkumar_mogha@sgs.com) : Ultrasonic studies of titanium (III) soaps in mixed organic solvents. Int J pure appl Chem 2007, 2(4), 387-90.

Several acoustic parameters viz., adiabatic compressibility, intermolecular free length, acoustic independence, molar sound velocity, molar sound compressibility and solvation number of titanium (III) soaps in mixed organic solvents (benzene + cyclohexane) were calculated at 35° and 45°C. The obtained results revealed important information about the structural change of the soaps in the non-aqueous media.

3 illus, 2 tables, 16 ref

014090   Suresh;Saini A;Sandhu J S (Chemistry Dep, Punjabi Univ, Patiala-147 002, Email: j_sandhu2002@yahoo.com) : CuSo₄.5H₂O catalyzed efficient one pot synthesis of α-amino nitriles. J Indian Chem Soc 2009, 86(3), 261-4.

α-Amino nitriles are synthesized in a one pot three component coupling of aldehydes, amines and trimethylsilyl cyanide using catalytic amount of CuSO₄.5H₂O at ambient temperature.

1 sch, 1 table, 16 ref

014089   Surat Kumar;Rastogi S N (Applied Sciences Dep, Faculty of Engineering, Dayalbagh Educational Institute, Dayalbagh, Agra, Email: kumar.surat@gmail.com) : Synthesis of m-(substituted aminohydroxypropoxy) phenylethanol-amines as potential biodynamic agents. Int J pure appl Chem 2007, 2(3), 313-18.

Aryoxypropanolamines and aryethanolamines are prepared and used as β-adrenergic receptor blockers in the treatment of hypertension. Report, incorporated the features of both of these kinds of β-adrenergic blockers in the lead structure and prepared these compounds using a novel bis-epoxide. This bis-epopxide was treated to generate m-(substituted aminohydroxypropoxy)phenylethanolamines. These compounds exhibited some promising stimulant and depressant activities.

2 illus, 1 table, 6 ref

014088   Sulekh Chandra;Singh D R;Agarwal H (Chemistry Dep, Zakir Husain College, Delhi Univ, J.L. Nehru Marg, New Delhi-110 002, Email: schandra_00@yahoo.com) : Novel Cu(II) selective PVC electrode based on 8,11,14-triaza-1,4-dioxo-5(6), 16(17)-dibenzocycloseptadecane as an ionophore. Int J pure appl Chem 2007, 2(4), 415-22.

A PVC membrane based copper (II) selective electrode was constructed using 8,11,14-triaza-1,4-dioxo,5(6),16(17)-dibenzocycloseptadecane (TSDOBCSD) as neutral carrier. The sensor exhibits a Nernstian response for Cu(II) ions over a wide concentration range of 1.0 x 10^-8- 10x 10^-1 M with a slope of 29.45 ± 0.5 mV/ decade, having detection limit of 8.0x 10^-7M (36 ppb). It has a relatively fast response time(< 10s for concentrations ≥ 1.0 x 10° M and < 15 s for concentration of > 10^-6 M) and can be used for 8 months without any considerable divergence in potentials. The proposed sensor revealed relatively good selectively and high sensitivity for Cu(II) over a bi-, tri- and tetravalent metal ions and could be used in a pH range of 3.5-8.0. It was successfully also used as an indicator electrode in potentiometer titration and in analysis of concentration of copper in various real samples.

5 illus, 4 tables, 35 ref

014087   Sulekh Chandra;Singh C K;Agarwal H (Chemistry Dep, Zakir Husain College, Delhi Univ, J.L. Nehru Marg, New Delhi-110 002, Email: schandra_00@yahoo.com) : Highly sensitive and selective chromium(III)-selective electrode based on a macrocyclic hexaazatricyclodecaene. Int J pure appl Chem 2007, 2(3), 347-52.

Attempt has been made to develop poly(vinyl chloride) based Cr³⁺ ion selective electrode using 2,5,11,14,19,20-hexaazatricyclo [13.3.1.1] cosa;l(19),2,4,6,8,10(20),11,13,15,17-decaene(HATCCD) with dibutyl phthalate as solvent mediator. The sensor exhibits a near Nernstian potential response at a wide concentration range (1.0 x 10^-1 x6.0x 10^-6M) with a detection limit of 10^-8M between pH 2.5-6.5 with a fast response time of < 8s. The selectivity coefficient values as determined by Match Potential Method (MPM) indicate excellent selectivity for Cr(III) ions over a large number of ions. Interference caused by common cations has been investigated in simulated mixtures containing high concentration level of interfering ions and the sensor was found to be tolerant against these cations. Proposed sensor exhibits adequate shelf-life (> 4 months) with good reproducibility. Quantification of Cr(III) in electroplating waste was successfully achieved using the proposed ISE.

4 illus, 4 tables, 26 ref