BITS Faculty Publications
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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.Item The synthesis of amino acid derived glycoconjugates and the investigation of their anti-inflammatory and analgesic properties(2014) Sah, Ajay KumarA series of 4,6-O-ethylidene-β-D-glucopyranosylamine derived glycoconjugates containing amino- and aromatic acids have been synthesized. All these molecules have been tested for their anti-inflammatory and analgesic activity on Wistar rat and Swiss Albino mice respectively. The anti-inflammatory studies were explored using a carrageenan induced paw oedema model while an acetic acid induced writhing model was adapted for the analgesic studies. All of the compounds exhibited anti-inflammatory and analgesic activity in the range of 63–84% and 86–94% respectively.