V. Alagarsamy, M. Rupeshkumar, K. Kavitha
Nov 1, 2008
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Influential Citations
34
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Quality indicators
Journal
European journal of medicinal chemistry
Abstract
Abstract A series of novel 1-substituted-4-(2-methylphenyl)-4 H -[1,2,4]triazolo[4,3- a ]quinazolin-5-ones were synthesized by the cyclization of 2-hydrazino-3-(2-methylphenyl)-3 H -quinazolin-4-one with various one carbon donors. The starting material 2-hydrazino-3-(2-methylphenyl)-3 H -quinazolin-4-one was synthesized from 2-methyl aniline by a novel innovative route. The title compounds were tested for their in vivo H 1 -antihistaminic activity on guinea pigs; all the tested compounds protected the animals from histamine-induced bronchospasm significantly. Compound 1-methyl-4-(2-methylphenyl)-4 H -[1,2,4]triazolo[4,3- a ]quinazolin-5-one ( II ) emerged as the most active compound of the series and it is more potent (72.45%) when compared to the reference standard chlorpheniramine maleate (71%). Compound II showed negligible sedation (11%) when compared to chlorpheniramine maleate (30%). Hence it could serve as the prototype molecule for further development as a new class of H 1 -antihistaminic agents.