Original articleDesign, synthesis and H1-antihistaminic activity of novel 1-substituted-4-(3-chlorophenyl)-[1,2,4] triazolo [4,3-a] quinazolin-5(4H)-ones

Add time:08/14/2019    Source:sciencedirect.com

In the present study a series of 1-substituted-4-(3-chlorophenyl)-[1,2,4] triazolo [4,3-a] quinazolin-5(4H)-ones were synthesized and screened for their H1-antihistaminic activity. The synthesized compounds were characterized by IR, 1H-NMR, mass spectral data and purity of the compounds was determined by elemental analysis. Antihistaminic activity of the title compounds was evaluated by histamine induced bronchoconstriction method in guinea pigs. Among the series, 4-(3-chlorophenyl)-1-methyl-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one (S5) was the most potent with the percentage protection of 69.65% and its potency is comparable to the reference drug chlorpheniramine maleate (70.09% protection). Interestingly the sedative property of compound S5 was found to be negligible (5.36%) when compared to chlorpheniramine maleate (34.92%).

We also recommend Trading Suppliers and Manufacturers of 4-(4-Chlorophenyl)-2-(methylthio)-3-thiophenecarbonitrile (cas 116526-42-2). Pls Click Website Link as below: cas 116526-42-2 suppliers

Prev:22-Thio-23,24-bisnor-5-cholen-3β-OL: An active site-directed inhibitor of cytochrome P450scc
Next:Stability of amorphous drug, 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H-pyridazin-3-one, in silica mesopores and measurement of its molecular mobility by solid-state 13C NMR spectroscopy)