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

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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1996-07, Vol.6 (13), p.1469-1474
Main Authors: Hirata, Terukage, Nomiyama, Jun, Sakae, Nobuya, Nishimura, Kouji, Yokomoto, Masaharu, Inoue, Satoshi, Tamura, Koichi, Okuhira, Masayasu, Amano, Hirotaka, Nagao, Yoshimitsu
Format: Article
Language:English
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Summary: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%). Syntheses and pharmacological properties of new acyliminothiadiazoline derivatives as AII antagonists including the selected candidate KRH-594 are described.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(96)00250-8