title: Generation of a small library of cyclodepsipeptide PF1022A analogues using a cyclization-cleavage method with oxime resin.
abstract: 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.
authors.affiliation: Discovery Research, Pharmacia Animal Health, Kalamazoo, MI 49001, USA. bhlee@pharmacia.com
authors.forename: Byung H
authors.initials: BH
authors.lastname: Lee
authors.forename: Fred E
authors.initials: FE
authors.lastname: Dutton
authors.forename: David P
authors.initials: DP
authors.lastname: Thompson
authors.forename: Eileen M
authors.initials: EM
authors.lastname: Thomas
mesh_terms: 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
chemical_list: D000871:Anthelmintics; D047630:Depsipeptides; D007202:Indicators and Reagents; D010091:Oximes; D019151:Peptide Library; D010456:Peptides, Cyclic; D012116:Resins, Plant; C075544:PF 1022A