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.