SYNTHESIS AND PHARMACOLOGICAL INVESTIGATION OF NOVEL<br /> THIAZOLOQUINAZOLINE AS NEW CLASS OF H1-ANTIHISTAMINIC AGENT
Journal Title: International Journal of Pharmacy and Technology - Year 2010, Vol 2, Issue 1
Abstract
A series of novel 6,7,8,9 tetra hydro-5H-5-(2'-hydroxy phenyl)-2-(4'-some substituted benzylidine)-3-(4-nitrophenyl amino) thiazolo quinazoline were synthesized the reaction with appropriate aromatic aldehydes and p –nitro aniline in the presence of anhydrous sodium acetate The starting material 6,7,8,9 tetra hydro-5H-5-(2'-hydroxy phenyl) thiazolo (2, 3-b) quinazolin-3(2H)- one 3 by a new innovative route with improved yield. When tested for their in vivo H-antihistaminic activity on conscious guinea pigs, all the test compounds significantly protected the animals from histamine induced bronchospasm. The compound 5b emerged as the most active compound of the series and it is more potent (73.93% protection) when compared to the reference standard, chlorpheniramine maleate (71% protection), it showed negligible sedation (10%) when compared to chlorpheniramine maleate (30%). Therefore compound 5b will serve as prototype molecule for further development as a new class of H1-antihistamines.
Authors and Affiliations
T. Panneer Selvam
Keywords
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