Synthesis and pharmacological investigation of novel 4-3-ethylphenyl-1-substituted-4H-1,2,4triazolo4,3-aquinazolin-5-ones as a new class of H1-antihistaminic agentsReport as inadecuate




Synthesis and pharmacological investigation of novel 4-3-ethylphenyl-1-substituted-4H-1,2,4triazolo4,3-aquinazolin-5-ones as a new class of H1-antihistaminic agents - Download this document for free, or read online. Document in PDF available to download.

Acta Pharmaceutica, Vol.59 No.1 March 2009. -

A series of novel 4-3-ethylphenyl-1-substituted-4H-1,2,4triazolo4,3-aquinazolin-5-ones 4a-j were synthesized by the cyclization of 3-3-ethylphenyl-2-hydrazino-3H-quinazolin-4-one 3 with various one-carbon donors. The starting material, compound 3, was synthesized from 3-ethyl aniline by a new innovative route with improved yield. When tested for their in vivo H1-antihistaminic activity on conscious guinea pigs, all test compounds protected the animals from histamine induced bronchospasm significantly. Compound 4-3-ethylphenyl-1-methyl-4H-1,2,4triazolo4,3-aquinazolin-5-one 4b emerged as the most active compound of the series and it is more potent 74.6 % protection compared to the reference standard chlorpheniramine maleate 71 % protection. Compound 4b shows negligible sedation 10 % compared to chlorpheniramine maleate 30 %. Therefore compound 4b can serve as the leading compound for further development of a new class of H1-antihistamines.

quinazolin-5-ones; sedation; H1-antihistaminic agents



Author: VEERACHAMY ALAGARSAMY - ; Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Fasalwadi, Sangareddy-502294, India K

Source: http://hrcak.srce.hr/



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