Acyliminothiadiazoline derivatives: New, highly potent, and orally active angiotensin II receptor antagonists

Article abstract of DOI:10.1016/S0960-894X(96)00250-8

Syntheses and pharmacological properties of a new series of acyliminothiadiazoline derivatives 1 are described. These compounds exhibited angiotensin II receptor antagonistic activities in vitro and in vivo. Among them, the compound 1g (KRH-594) showed the strongest antihypertensive action in renal hypertensive rats after oral administration, and its oral bioavailability in dogs was also found to be high (73%).