Department of Chemistry
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Item Thiazolidinyl-triazinoquinazolines as potent anti-inflammatory agents(NISCAIR, 2001-04) Bajaj, KiranSome 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.Item Synthesis and anti-inflammatory, analgesic, ulcerogenic and cyclooxygenase activities of novel quinazolinyl-2-pyrazolines(NISCAIR, 2002-03-13) Bajaj, KiranItem Synthesis of some newer derivatives of 2-amino benzoic acid as potent anti-inflammatory and analgesic agents.(PMC, 2003-11-01) Bajaj, KiranDiazotization 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.Item Some new 2,3,6-trisubstituted quinazolinones as potent anti-inflammatory, analgesic and COX-II inhibitors(Elsiever, 2003-11-17) Bajaj, KiranVarious 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.Item Synthesis of acridinyl-thiazolino derivatives and their evaluation for anti-inflammatory, analgesic and kinase inhibition activities(Elsiever, 2005-07-01) Bajaj, KiranVariety of N-(4-phenyl-3-(2′,3′,4′(un)substituted phenyl)thiazol-2(3H)-ylidene)-2,4(un)substituted acridin-9-amine (4a–o) and 1-[(2,4-(un)substituted acridin-9-yl)-3-(4-phenyl-3-(2′,3′,4′(un)substituted phenyl)thiazol-2(3H)-ylidene)]isothiourea (5a–h) derivatives have been synthesized by condensation of 4-phenyl-3-(2′,3′,4′(un)substituted phenyl)thiazol-2(3H)-imine (3a–g) with 9-chloro-2,4-(un)substituted acridine (1a–c) and 9-isothiocyanato-2,4-(un)substituted acridine (2a–d), respectively. All these compounds were characterized by correct 1H NMR, FT-IR, MS and elemental analyses. These compounds were screened for anti-inflammatory, analgesic and kinase (CDK1, CDK5 and GSK3) inhibition activities. Some compounds exhibited good anti-inflammatory (25–32%) and potent analgesic (50–75%) activities, at 50 mg/kg p.o. A compound, 4o (R1 = H, R2 = OCH3, R3 = CH3, R4 = CH3, R5 = H) exhibited moderate CDK1 (IC50 = 8.5 μM) inhibition activity.