Department of Chemistry
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Item Synthesis and anti-inflammatory, analgesic, ulcerogenic and cyclooxygenase activities of novel quinazolinyl-2-pyrazolines(NISCAIR, 2002-03-13) Bajaj, KiranItem 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.