Substituted phenylacetylguanidines: a new class of antihypertensive agents.
The synthesis of a new series of phenylacetylguanidines is described. Several of them exhibited high antihypertensive activity in the rat. The most potent member of the series is N-amidino-2-(2,6-dichlorophenyl)acetamide hydrochloride [2,6-dichlorophenylacetylguanidine hydrochloride, compound 19], which is now in clinical study under the clinical code number BS 100-141. The structure-activity relationships in this class of compounds are discussed.
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D005260:Female; D006146:Guanidines / Q000138:chemical synthesis* / Q000627:therapeutic use; D006973:Hypertension / Q000188:drug therapy; D008722:Methods; D010648:Phenylacetates / Q000138:chemical synthesis / Q000627:therapeutic use; D051381:Rats; D013329:Structure-Activity Relationship
D000959:Antihypertensive Agents; D006146:Guanidines; D010648:Phenylacetates