Abstract
A series of novel 2-phenyl-3-[2-(substituted amino) ethylamino] quinazolin-4(3H)-ones was synthesized by the nucleophilic substitution of 3-(2-bromo ethylamino)-2-phenyl quinazolin-4(3H)-one with various amines. The starting material, 3-(2-bromo ethylamino)-2-phenyl quinazolin-4(3H)-one, was synthesized from anthranilic acid by a multistep synthesis. All the title compounds were tested for their in vivo H1-antihistaminic activity on conscious guinea pigs at the dose level of 10 mg/kg using chlorpheniramine as the standard drug. The results of the biologic activity revealed that all the test compounds protected the animals from histamine-induced bronchospasm significantly. Compound 2-phenyl-3-[2-(piperazinyl) ethylamino] quinazolin-4(3H)-one (S3) emerged as the most active compound of the series (73.67 % protection) when compared to the standard chlorpheniramine (70.09 % protection). Interestingly, compound S3 shows negligible sedation (8.21 %) compared to chlorpheniramine maleate (29.58 %). Therefore, compound S3 can serve as the lead molecule for further development into a new class of H1-antihistaminic agents.
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