期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 15, 期 12, 页码 4009-4015出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.04.001
关键词
quinazoline; pyrimidine; antihistamine
A series of novel 1-substituted-4-benzyl-4H-[1,2,4]triazolo[4,3-a]quinazolin-5-ones were synthesized by the cyclization of 2-hydrazino-3-benzyl-3H-quinazolin-4-one with various one-carbon donors. The starting material 2-hydrazino-3-benzyl-3H-quinazolin-4-one was synthesized from benzylamine by a new innovative route. When tested for their in vivo H-1-antihistaminic activity on guinea pigs, all the test compounds protected the animals from histamine induced bronchospasm significantly. The compound Imethyl-4-benzy1-4H- [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 (percent protection 76%) when compared to the reference standard chlorpheniramine maleate (percent protection 71%). Compound II showed negligible sedation (7%) when compared to chlorpheniramine maleate (30%). Hence it could serve as prototype molecule for further development as a new class of H1-antihistamines. (C) 2007 Elsevier Ltd. All rights reserved.
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