Synthesis and evaluation of backbone/amide-modified analogs of leualacin

Authors
Hu, MK Yang, FC Chou, CC Yen, MH
Citation
Mk. Hu et al., Synthesis and evaluation of backbone/amide-modified analogs of leualacin, BIOORG MED, 9(4), 1999, pp. 563-568
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
4
Year of publication
1999
Pages
563 - 568
Database
ISI
SICI code
0960-894X(19990222)9:4<563:SAEOBA>2.0.ZU;2-R
Abstract
Leualacin (1), a cyclic depsi-pentapeptide, and its backbone/amide-modified analogs 2-4 were synthesized. Amide analogue 3 exhibited stronger vasodila tory effects. It also strongly inhibited collagen- and arachidonic acid (AA )induced platelet aggregations with IC(50)s of 0.6 mu M and 2.0 mu M, respe ctively (C) 1999 Elsevier Science Ltd. All rights reserved.