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Chimeric cyclodepsipeptides as mimetics for the anthelmintic PF1022A.

Authors
  • Dyker, Hubert
  • Harder, Achim
  • Scherkenbeck, Jürgen
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Dec 20, 2004
Volume
14
Issue
24
Pages
6129–6132
Identifiers
PMID: 15546743
Source
Medline
License
Unknown

Abstract

In the anthelmintic cyclooctadepsipeptide PF1022A (1) didepsipeptide units have been exchanged for the beta-turn mimetics (D)-Pro-(L)-Pro and BTD (7) in order to elucidate the functional role of the depsipeptide backbone. Compounds 12 and 14 are the first PF1022A analogues in which a substantial part of the PF1022A backbone has been replaced with an improvement of anthelmintical activity. Preliminary structure-activity relationships suggest a symmetric conformation to be the biological active one.

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