Design and Synthesis of Novel 3-(4-Chlorophenyl)-2-(3-Substituted Propyl Thio) Quinazolin-4-(3H)-ones as a New Class of H₁-Antihistaminic Agents

Abstract

A series of novel 3-(4-chlorophenyl)-2-(3-substituted propyl) quinazolin-4-(3H)-ones have been synthesized and tested for their in vivo H₁-antihistaminic activity on conscious guinea pigs. All the test compounds have protected the animals from histamine induced bronchospasm significantly. Compound 3-(4-chlorophenyl)-2-(3-(4-methylpiperazin-1-yl) propylthio) quinazolin-4(3H)-one (PC5) emerged as the most active compound (77.53% protection) of the series when compared to the reference standard chlorpheniramine maleate (70.09% protection). Compound PC5 shows negligible sedation (6.16%) compared to chlorpheniramine maleate (29.58%). Therefore, compound PC5 can serve as the lead molecule for further development into a new class of H₁-antihistaminic agents.

Key words

quinazolin-4-ones - sedation - H₁-antihistaminic activity

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