1-Oxacephem-based human chymase inhibitors: Discovery of stable inhibitorsin human plasma

Authors
Aoyama, Y Uenaka, M Konoike, T Iso, Y Nishitani, Y Kanda, A Naya, N Nakajima, M
Citation
Y. Aoyama et al., 1-Oxacephem-based human chymase inhibitors: Discovery of stable inhibitorsin human plasma, BIOORG MED, 10(21), 2000, pp. 2403-2406
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
21
Year of publication
2000
Pages
2403 - 2406
Database
ISI
SICI code
0960-894X(20001106)10:21<2403:1HCIDO>2.0.ZU;2-0
Abstract
1-Oxacephem derivatives were evaluated as a novel series of chymase inhibit ors. The structure-activity relationship studies of 1-oxacephems led to com pounds 15, which exhibited 27 nM inhibition of human chymase and improvemen t of stability in human plasma (t(1/2) 1.5 h), (C) 2000 Elsevier Science Lt d. All rights reserved.