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 on an in vitro assay.
Lee
Byung H
BH
Discovery Research, Pharmacia Animal Health, Kalamazoo, MI 49001, USA. bhlee@pharmacia.com
Dutton
Fred E
FE
Thompson
David P
DP
Thomas
Eileen M
EM
D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D003500:Cyclization; D047630:Depsipeptides; D006189:Haemonchus; D007202:Indicators and Reagents; D010091:Oximes / Q000737:chemistry*; D019151:Peptide Library; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D012116:Resins, Plant; D013329:Structure-Activity Relationship
D000871:Anthelmintics; D047630:Depsipeptides; D007202:Indicators and Reagents; D010091:Oximes; D019151:Peptide Library; D010456:Peptides, Cyclic; D012116:Resins, Plant; C075544:PF 1022A