The present study deal with the synthesis of novel Dihydropyrimidinone derivatives from the reaction of N-substituted piperazine and substituted Dihydropyrimidinone in presence of Dimethyl formamide(DMF).All the compounds were characterized using IR,1H-NMR,MS and elementary analysis. They were screened for their antihypertensive activity. Result revealed that compound which contains SO2 between piperazine and DHPM skeletal (7g) was most active compound among the all 9 compounds. Compound 7g which showed nearer to similar activity to standard drug prazosin. Other compound showed good to moderate activity. Structure activity relationship of these compounds showed that piperazine ring should be necessary for the a1A adrenergic receptor blocking activity. Substituted primary aromatic amine attached to Dihydropyrimidinone ring instead of piperazine ring resulted in very less activity.
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