Synthesis and anti-inflammatory activity of some new 2,3-disubstituted-6-monosubstituted-quinazolin-4(3<i>H</i>)-ones

2642-2646Some new quinazolinone derivatives, 3-(substituted phenyl)-2-(substituted phenylchalconylaminoazetidinon-2'-yl)-6- monosubstitutedquinazolin-4(3H)-ones have been synthesized by the reaction of 3-(substituted phenyl)-2-(substituted phenylchalconylhydra zinomethyl)-6-monosubstituted-quinazolin-4(3H)-ones with acetyl chloride in the presence of triethylamine. All the compounds or this series have been evaluated for their anti-inflammatory activity against carrageenan induced oedema in albino rats. The activity of the most active member of this series i.e. 3-(o-methoxyphenyl)-2-(p-dimethylaminophenylchal conylaminoazetidinon-2'-yl) quinazolin-4(3H)-one has been studied in detial and is compared with phenylbutazone. Interestingly this compound exhibits better anti -inflammatory activity and lower ulcerogenic liability than phenylbutazone and its toxicity is also quite low

Thiazolidinyl-triazinoquinazolines as potent anti-inflammatory agents

307-312Some 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