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

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

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1469 - 1474 (1996)

Update date:2022-08-06

Topics:

Authors:

Hirata, Terukage

Nomiyama, Jun

Sakae, Nobuya

Nishimura, Kouji

Yokomoto, Masaharu

Inoue, Satoshi

Tamura, Koichi

Okuhira, Masayasu

Amano, Hirotaka

Nagao, Yoshimitsu

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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%).

Full text of DOI:10.1016/S0960-894X(96)00250-8

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