M Gobinath1 
,
N Subramanian2,
V Alagarsamy3,
S Nivedhitha1,
V Raja Solomon3
For correspondence:- M Gobinath Email: drvalagarsamy@gmail.com Tel:+919246425702
Received: 23 January 2014 Revised: 23 December 2014 Published: 28 February 2015
Citation: Gobinath M, Subramanian N, Alagarsamy V, Nivedhitha S, Solomon VR. Synthesis of 1-substituted-4-(pyridin-4-yl) [1,2,4] triazolo [4,3-a] quinazolin-5(4H)-ones as a new class of H1-antihistaminic agents. Trop J Pharm Res 2015; 14(2):271-277 doi: 10.4314/tjpr.v14i2.12
© 2015 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..
Purpose: To synthesize a new series of 1-substituted-4-(pyridin-4-yl) [1,2,4] triazolo[4,3-a]quinazolin-5(4H)-ones and evaluate them for H1-antihistaminic activity with negligible side effects in guinea pigs.
Methods: The synthesized compounds were characterized by Infrared spectroscopy (IR), proton nuclear magnetic resonance (1H-NMR) and mass spectrometry (MS) data. The purity of the compounds was determined by elemental analysis. The antihistaminic activity of the compounds was evaluated in guinea pigs by histamine-induced bronchoconstriction method.
Results: Among the series, 1-methyl-4-(pyridin-4-yl) [1,2,4] triazolo [4,3-a] quinazolin-5(4H)-one (S5) was the most potent with 72.85 % protection and its potency was comparable to that of the reference, chlorpheniramine maleate (70.09 %). Interestingly, the sedative property of compound S5 was negligible (5.09 %) when compared to chlorpheniramine maleate (29.58 %).
Conclusion: Compound S5 can serve as a lead molecule for further development into a new class of H1-antihistaminic agents.
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