Generation of a small library of cyclodepsipeptide PF1022A analogues using a cyclization-Cleavage method with oxime resin

Generation of a small library of cyclodepsipeptide PF1022A analogues using a cyclization-Cleavage method with oxime resin

N-Methyloctadepsipeptides attached to an oxime resin were cyclized by heating them in refluxing ethyl acetate for 2 days to give cyclodepsipeptide PF1022A analogues. By using this method, we generated a small library of PF 1022A analogues ( 2), several of which possessed anthelmintic activity, based...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2002-02, Vol.12 (3), p.353-356
Hauptverfasser: Lee, Byung H, Dutton, Fred E, Thompson, David P, Thomas, Eileen M
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Anthelmintics - chemical synthesis
Anthelmintics - chemistry
Anthelmintics - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Biological and medical sciences
Chromatography, High Pressure Liquid
Cyclization
Depsipeptides
Haemonchus
Indicators and Reagents
Medical sciences
Oximes - chemistry
Peptide Library
Peptides, Cyclic - chemical synthesis
Peptides, Cyclic - chemistry
Peptides, Cyclic - pharmacology
Pharmacology. Drug treatments
Resins, Plant
Structure-Activity Relationship
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Zusammenfassung:N-Methyloctadepsipeptides attached to an oxime resin were cyclized by heating them in refluxing ethyl acetate for 2 days to give cyclodepsipeptide PF1022A analogues. By using this method, we generated a small library of PF 1022A analogues ( 2), several of which possessed anthelmintic activity, based on an in vitro assay. N-Methyloctadepsipeptides attached to an oxime resin were cyclized by heating them in refluxing ethyl acetate for 2 days to give cyclodepsipeptide PF1022A analogues. Using this method, we generated a small library of PF1022A analogues ( 2), several of which possessed anthelmintic activity, based on an in vitro assay.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00748-X