BITS Faculty Publications

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End date: 2009Subject: search.filters.subject.Chemistry

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    Thiazolidinyl-triazinoquinazolines as potent anti-inflammatory agents
    (NISCAIR, 2001-04) Bajaj, Kiran
    Some new 5-(5'-substituted-aryl-2'-oxo-4'-thiazolidin-1'-yl)amino-4-phenyl-2-methyl-10-bromo-[1,2,4] triazino[2 ,3-c]quinazolines have been synthesized by [1,5]cyclocondensation of thiolactic acid with 5-arylidene hydrazino-4-phenyl-2-methyl-10-bromo-[1,2,4] triazino [2 ,3-c] quinazolines. All the compounds of the series have been screened for their anti-inflammatory activity. The most potent compound of the series 5-(5'-p-dimethylaminophenyl-2'-oxo-4'-thiazolidin-1'-yl) amino-4-phenyl-2-methyl-10-bromo-[1,2,4] triazino[2,3-c]quinazolines has shown 48.93% activity at a dose of 50 mg/kg p.o. The structures of the products have been delineated by chemical reactions, elemental analysis and spectral studies.
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    Synthesis of 1,5-benzothia/oxazepines as potent neuroleptic agents
    (NISCAIR, 2003-05) Bajaj, Kiran
    Some new 2-(4'-oxo-2'-substitutedaryl-thiazolidinyl)iminomethyl-1 ,5-benzothialoxazepin-4(5H)-ones 5a-d/5a'-d' and 2-(4'-oxo-3'-chloro-2'-substitutedaryl-azetidinyl)-imino-methyl-l ,5-benzothialoxazepin-4(5H)-ones 6a-dl6a' -d' have been synthesized starting from 2-aminobenzenethioVphenol and evaluated for their neuroleptic activity. The structures of the synthesized compounds are confirmed by IR, 1H NMR and mass spectrometery and also by chemical methods.
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    Synthesis of Newer Indolyl/ Phenothiazinyl Substituted 2-Oxo/ Thiobarbituric Acid Derivatives as Potent Anticonvulsant Agents
    (Thieme, 2003) Bajaj, Kiran
    2-Amino-5-(heteroarylmethylene)-1,3,4-oxadiazoles/thiadiazoles 7−10 were synthesized by cyclisation of 1-(heteroarylacetyl)semicarbazides/thiosemicarbazides 3−6. 5-(2’-Heteroarylmethylene-5’-aminomethylene-1’, 3’, 4’-oxadiazol-2’-yl/ thiadiazol-2’-yl)-2-oxo/thiobarbituric acids 11−18 were synthesized by condensation of compounds 7−10 at the 5th position of 2-oxo/thiobarbituric acids. The newly synthesized compounds showed anticonvulsant activity ranging from 50–90 % (seizures protection). Compound 18 (5-(2’-phenothiazinylmethylene-5’-aminomethylene-1’,3’,4’-thiadiazol-2’-yl)-2-thiobarbituric acid) showed maximum activity being more potent than the reference drug phenytoin sodium (CAS 630-93-3)
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    Synthesis of some new benzothia/oxazepinyl indoles as an antipsychotic agents
    (NISCAIR, 2003-07) Bajaj, Kiran
    Some new 3-(2'-substitutedaryl -2',3'-dihydro-1 ',5'-benzothia/oxazepin-4'-yl)indoles 3a-h, 3-(2'-substitutedary 1-3'substitutedarylaminomethylene-2' ,3'-dihydro-1',5'-benzothia/oxazepin-4'-yl)indoles 4a-p and 3-(2'-substitutedary 1-3'substitutedarylazo- 2',3'- dihydro-1',5'- benzothia/oxazepin-4'-yl)indoles 5a-p have been synthesized and evaluated for antipsychotic activity. 3-[2'-( 4"-N,N-dimethylphenyl)-3' -arylaminomethylene-2',3'-dihydro-1 ,5-benzothiazepin-4'-yl] indole 4i showes most promising antipsychotic activity. The structures of all the compounds were determined by IR,1H NMR and mass spectrometry.
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    Newer Substituted Benzoxazepinylquinazolinones as Potent Antipsychotic and Anticonvulsant Agents
    (Thieme, 2003) Bajaj, Kiran
    3-Amino-[2’-substitutedaryl-3’-substitutedarylaminomethylene-2’,3’-dihydro-1’,5’-benzoxazepin-4’-yl]-2-methylquinazolin-4(3H)-ones 11−18 and 3-amino-[2’-substituted aryl-3’-substitutedaryl-azo-2’,3’-dihydro-1’,5’-benzoxazepin-4’-yl]-2-methyl-quinazolin-4(3H)-ones 19− 26 were synthesized from 3-amino-[2’-substitutedaryl-2’,3’-dihydro-1’,5’-benzoxazepin-4’-yl]-2-methyl-quinazolin-4(3H)-ones 7−10 by Mannich’s reaction and by diazotisation, respectively, on the 3rd position of the benzoxazepine ring of the compounds 7−10. The newly synthesized compounds showed potent antipsychotic and anticonvulsant activities.
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    Synthesis of some newer derivatives of 2-amino benzoic acid as potent anti-inflammatory and analgesic agents.
    (PMC, 2003-11-01) Bajaj, Kiran
    Diazotization of N-benzylidene anthranilic acids 1a-1n at pH 9 yielded N-[alpha-(phenylazo) benzylidene] anthranilic acids 2a-2n and at pH 3 yielded N-benzylidene-5-(phenylazo) anthranilic acids 3a-3n. When compounds 3a-3n were treated with thioglycolic/thiolactic acid in the presence of anhydrous ZnCl(2), 2-(4-oxo-2-phenylthiazolidin-3-yl)-5-(phenylazo) benzoic acids 4a-4n were afforded. The newly synthesized compounds were screened for their anti-inflammatory and analgesic activities and were compared with standard drugs, aspirin and phenylbutazone. Out of the compounds studied, the most active compound 4n showed more potent activity than the standard drugs at all doses tested.
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    Some new 2,3,6-trisubstituted quinazolinones as potent anti-inflammatory, analgesic and COX-II inhibitors
    (Elsiever, 2003-11-17) Bajaj, Kiran
    Various 2-(substitutedphenylmethyleneimino)aminoacetylmethylene-3-(2′-substitutedindol-3′-yl)-halosubstituted-4(3H)quinazolinones (5a–5i) and 2-(substituted phenylaminomethyleneacetyl-4′-oxo-1′-thiazolidinyl-3-(2″-substitutedindol-3″-yl) 4(3H)-quinazolinones (6a–6i) have been synthesized in the present studies. The structure of these compounds have been elucidated by elemental (C, H, N) and spectral (IR, 1H NMR and mass) analysis. Furthermore, above said compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic activities and acute toxicity study. Compound 6d was found to be most potent. Compound exihibiting less ulcerogenic liability and ALD50 >2000 mg/kg po. Some 2-(substitutedphenylmethyleneimino)aminoacetylmethylene-3-(2′-substitutedindol-3′-yl)-halosubstituted-4(3H)quinazolinones (5a–5i) and 2-(substituted phenylaminomethyleneacetyl-4′-oxo-1′-thiazolidinyl-3-(2″-substitutedindol-3″-yl)-4(3H)-quinazolinones (6a–6i) have been synthesized. Compound 2-(o-Methoxyphenylaminomethylacetyl-4′-oxo-1′-thiazolidinyl)-3-(indol-3″-yl)-6-iodo-4(3H)-quinazolinone (6d) was found to be the most potent compound of the present study.
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    Synthesis and psychotropic evaluation of some new N-substitutedbenzothia/oxazepinylphenothiazines
    (NISCAIR, 2004-01) Bajaj, Kiran
    A number of N-[2-substitutedaryl-3-substitutedarylaminomethylene-2, 3-dihydro- 1, 5-benzothia/oxazepin-4-yl] phenothiazines 4a-p and 4a'-p' have been synthesized from N-[2-substitutedaryl-2, 3-dihydro-1, 5-benzothia/ oxazepin-4-yl]phenothiazines by Mannich reaction, on the 3rd position of benzothia/oxazepine ring. The structure of these compounds have been confirmed by IR, 1H NMR and Mass analysis. The newly synthesized compounds have been evaluated for their psychotropic activities and acute toxicity studies. Compound 4i is found to be most potent compound of this series.
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    Synthesis and pharmacological evaluation of newer substituted benzoxazepine derivatives as potent anticonvulsant agents
    (Elsiever, 2004-04) Bajaj, Kiran
    A series of 2-substitutedphenyl-3-(substitutedphenylamino)methyl-2,3-dihydro-4-diphenylamino-1,5-benzoxazepines (4a–4p) and 2-substitutedphenyl-3-substitutedphenylazo-2,3-dihydro-4-diphenylamino-1,5-benzoxazepines (5a–5p) have been synthesized from 2-substitutedphenyl-2,3-dihydro-4-diphenylamino-1,5-benzoxazepines (3a–3d) by the Mannich reaction and diazotization reaction, respectively. All these compounds were screened, in vivo, for their anticonvulsant activity and acute toxicity studies. Compounds 4p and 5p were found to be most potent compounds of this series and were compared with the reference drug phenytion sodium, lamotrigine and sodium valproate. The structures of these compounds have been established by IR, 1H NMR and mass spectroscopic data.