期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 23, 页码 8324-8333出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.09.067
关键词
Pseudopterosins; Anti-inflammatory; Mouse-ear assay; Catechol glycosides
资金
- Swiss National Science Foundation
- DFG, Germany
- California Sea Grant Program
- National Sea Grant Program
The synthesis and in vivo anti-inflammatory activity of a series of pseudopterosin analogues are presented. Synthetic tricyclic catechol aglycons with different substitution patterns were monofucosylated or -xylosylated. Anti-inflammatory activity was conserved over a wide range of structural modifications. The most active synthetic compound 33 reduced phorbol myristate acetate (PMA)-induced inflammation in the mouse ear by 72% at 50 mu g/ear. This corresponds to 80% of the activity of natural pseudopterosin A. (C) 2010 Elsevier Ltd. All rights reserved.
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