Title of article :
Synthesis of 4-butyl-1-substituted-4H-[1,2,4]triazolo[4,3-a]quinazolin-5-ones as new class of H1-antihistaminic agents
Author/Authors :
V. Alagarsamy، نويسنده , , D. Shankar، نويسنده , , S. Murugesan، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Pages :
6
From page :
173
To page :
178
Abstract :
A series of novel 4-butyl-1-substituted-4H-[1,2,4]triazolo [4,3-a] quinazolin-5-ones were synthesized by the cyclization of 3-butyl-2-hydrazino-3H-quinazolin-4-one with various one carbon donors. The starting material 3-butyl-2-hydrazino-3H-quinazolin-4-one was synthesized from butyl amine by a new innovative route. When tested for their in vivo H1-antihistaminic activity on conscious guinea pigs, all the test compounds protected the animals from histamine induced bronchospasm significantly. Compound 4-butyl-1-methyl-4H-[1,2,4]triazolo[4,3-a] quinazolin-5-one (II) emerged as the most active compound of the series and it is equipotent (71.91% protection) when compared to the reference standard chlorpheniramine maleate (71% protection). Compound II show negligible sedation (9%) when compared to chlorpheniramine maleate (30%).
Keywords :
sedation , Quinazolin-5-ones , H1-Antihistaminic agents
Journal title :
Biomedicine and Pharmacotherapy
Serial Year :
2008
Journal title :
Biomedicine and Pharmacotherapy
Record number :
478056
Link To Document :
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