کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2525692 | 1119624 | 2008 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis of 4-butyl-1-substituted-4H-[1,2,4]triazolo[4,3-a]quinazolin-5-ones as new class of H1-antihistaminic agents Synthesis of 4-butyl-1-substituted-4H-[1,2,4]triazolo[4,3-a]quinazolin-5-ones as new class of H1-antihistaminic agents](/preview/png/2525692.png)
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%).
Journal: Biomedicine & Pharmacotherapy - Volume 62, Issue 3, March 2008, Pages 173–178