Syntheses and pharmacological properties of a new series of acyliminot
hiadiazoline derivatives 1 are described. These compounds exhibited an
giotensin II receptor antagonistic activities in vitro and in vivo. Am
ong them, the compound 1g (KRH-594) showed the strongest antihypertens
ive action in renal hypertensive rats after oral administration, and i
ts oral bioavailability in dogs was also found to be high (73%). Copyr
ight (C) 1996 Elsevier Science Ltd