Title of article :
Acyliminothiadiazoline derivatives: New, highly potent, and orally active angiotensin II receptor antagonists
Author/Authors :
Terukage Hirata، نويسنده , , Jun Nomiyama، نويسنده , , Nobuya Sakae، نويسنده , , Kouji Nishimura، نويسنده , , Masaharu Yokomoto، نويسنده , , Satoshi Inoue، نويسنده , , Koichi Tamura، نويسنده , , Masayasu Okuhira، نويسنده , , Hirotaka Amano، نويسنده , , Yoshimitsu Nagao، نويسنده ,
Abstract :
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%).
