4,5,6,7-TETRAHYDRO-8-OXO-CYCLOHEPTIMIDAZOLES - A NEW CLASS OF POTENT NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

Authors
YANAGISAWA T UEYAMA N KAWAI T SONEGAWA M BABA H MOCHIZUKI S KOZAKAI K TOMIYAMA T
Citation
T. Yanagisawa et al., 4,5,6,7-TETRAHYDRO-8-OXO-CYCLOHEPTIMIDAZOLES - A NEW CLASS OF POTENT NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 3(8), 1993, pp. 1559-1564
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
8
Year of publication
1993
Pages
1559 - 1564
Database
ISI
SICI code
0960-894X(1993)3:8<1559:4-ANCO>2.0.ZU;2-8
Abstract
1,4,5,6,7,8-hexahydrocycloheptimidazoles and 4,5,6,7-tetrahydro-8-oxo- cycloheptimidazolones were synthesized as potential angiotensin-II (AI I) receptor antagonists. One of these, 11c, KT3-671, was more potent t han losartan with a pA2 value of 10.04 and AT1 specific with an IC50 O f 0.8 nM. In an in vivo study, it had long lasting action on blood pre ssure in RHR rat at a dose of 3 mg/kg.