Preparation and immunosuppressive activity of 32-(O)-acylated and 32-(O)-thioacylated analogues of ascomycin

Authors
Hersperger, R Schuler, W Zenke, G
Citation
R. Hersperger et al., Preparation and immunosuppressive activity of 32-(O)-acylated and 32-(O)-thioacylated analogues of ascomycin, BIOORG MED, 9(2), 1999, pp. 227-232
Citations number
21
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
2
Year of publication
1999
Pages
227 - 232
Database
ISI
SICI code
0960-894X(19990118)9:2<227:PAIAO3>2.0.ZU;2-D
Abstract
A series of 32-(O)-acylated and 32-(O)-thioacylated derivatives of the anti biotic ascomycin (1) have been synthesized. These readily accessible analog ues exhibit potent immunosuppressive activity in vitro, as measured by an i nterleukin-2 reporter gene assay and the mixed lymphocyte reaction. Such mo lecules are expected to have a therapeutic potential in chronic inflammator y diseases of the airways such as asthma. (C) 1999 Elsevier Science Ltd. Al l rights reserved.