Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors

Authors
Aoyama, Y Uenaka, M Konoike, T Iso, Y Nishitani, Y Kanda, A Naya, N Nakajima, M
Citation
Y. Aoyama et al., Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors, BIOORG MED, 10(21), 2000, pp. 2397-2401
Citations number
20
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
21
Year of publication
2000
Pages
2397 - 2401
Database
ISI
SICI code
0960-894X(20001106)10:21<2397:SASROA>2.0.ZU;2-Q
Abstract
1-Oxacephem derivatives were synthesized and evaluated as a novel series of chymase inhibitors. Structure-activity relationship studies of 1-oxacephem s led to compound 34, which exhibited 6 nM inhibition of human chymase and high selectivity for human chymase compared to other serine enzymes. (C) 20 00 Elsevier Science Ltd. All rights reserved.