Some new 2,3,6-trisubstituted quinazolinones as potent anti-inflammatory, analgesic and COX-II inhibitors

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, H-1 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 ALD(50) > 2000 mg/kg po. (C) 2003 Elsevier Ltd. All rights reserved.