NDLI: Synthesis and pharmacological investigation of novel 4-(3-ethylphenyl)-1-substituted-4H-[1,2,4]triazolo[4,3-a] quinazolin-5-ones as a new class of H1-antihistaminic agents.

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Synthesis and pharmacological investigation of novel 4-(3-ethylphenyl)-1-substituted-4H-[1,2,4]triazolo[4,3-a] quinazolin-5-ones as a new class of H1-antihistaminic agents.

Content Provider	Semantic Scholar
Author	Alagarsamy, Veerachamy Kavitha, Kunchu Rupeshkumar, Mani Solomon, Viswas Raja Kumar, Jaya Kumar, Dinakaran Sathesh Sharma, Hemant Kumar
Copyright Year	2009
Abstract	A series of novel 4-(3-ethylphenyl)-1-substituted-4H-[1,2,4] triazolo[4,3-a]quinazolin-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 - [1,2,4]triazolo[4,3-a]quinazolin-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.
Starting Page	97
Ending Page	106
Page Count	10
File Format	PDF HTM / HTML
DOI	10.2478/v10007-009-0003-1
PubMed reference number	19304562
Journal	Medline
Volume Number	59
Issue Number	1
Alternate Webpage(s)	https://www.degruyter.com/downloadpdf/j/acph.2009.59.issue-1/v10007-009-0003-1/v10007-009-0003-1.pdf
Alternate Webpage(s)	https://doi.org/10.2478/v10007-009-0003-1
Journal	Acta pharmaceutica
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article

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