ACYLIMINOTHIADIAZOLINE DERIVATIVES - NEW, HIGHLY POTENT, AND ORALLY-ACTIVE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

Authors
HIRATA T NOMIYAMA J SAKAE N NISHIMURA K YOKOMOTO M INOUE S TAMURA K OKUHIRA M AMANO H NAGAO Y
Citation
T. Hirata et al., ACYLIMINOTHIADIAZOLINE DERIVATIVES - NEW, HIGHLY POTENT, AND ORALLY-ACTIVE ANGIOTENSIN-II RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 6(13), 1996, pp. 1469-1474
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
13
Year of publication
1996
Pages
1469 - 1474
Database
ISI
SICI code
0960-894X(1996)6:13<1469:AD-NHP>2.0.ZU;2-3
Abstract
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