A NEW CLASS OF DIACIDIC NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

A novel series of heterocyclic compounds I bearing two acidic function alities, a carboxyl group and a tetrazole ring, was prepared and evalu ated for in vitro and in vivo angiotensin II (AII) antagonistic activi ty. These compounds showed significantly more potent AII antagonistic activities than the parent compounds without the carboxyl groups. This structure-activity relationship (SAR) study revealed the importance o f the carboxyl group attached to the heterocyclic moieties especially for insurmountable antagonism and enhancement of in vivo (po) activity .