Design, synthesis and H1-antihistaminic activity of novel 1-substituted-4-(3-chlorophenyl)-[1,2,4] triazolo [4,3-a] quinazolin-5(4H)-ones
作者： Manavalan Gobinath , Natesan Subramanian , Veerachamy Alagarsamy
DOI: 10.1016/J.JSCS.2012.02.006
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摘要: Abstract In the present study a series of 1-substituted-4-(3-chlorophenyl)-[1,2,4] triazolo [4,3- ] quinazolin-5(4 H )-ones were synthesized and screened for their 1 -antihistaminic activity. The compounds characterized by IR, H-NMR, mass spectral data purity was determined elemental analysis. Antihistaminic activity title evaluated histamine induced bronchoconstriction method in guinea pigs. Among series, 4-(3-chlorophenyl)-1-methyl-[1,2,4]triazolo[4,3-a]quinazolin-5(4 )-one ( S5 ) most potent with percentage protection 69.65% its potency is comparable to reference drug chlorpheniramine maleate (70.09% protection). Interestingly sedative property compound found be negligible (5.36%) when compared (34.92%).
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