title: Structure-activity relationship of anthelmintic cyclooctadepsipeptides.
abstract: The relationship between cyclooctadepsipeptides and their anthelmintic efficacy was examined by converting the natural products, PF1022A, PF1022E and PF1022H. Some analogues substituted at the para position of the phenyllactate moiety showed higher or equivalent activity against the parasitic nematode, Ascaridia galli in chicken when compared with the parent compounds. It is suggested that lipophilicity and the polar surface area, in addition to structural requirements of the derivatives, influenced the anthelmintic efficacy in vivo.
authors: Department of Electronic Chemistry, Interdisciplinary Graduate School of Science and Engineering, Tokyo Institute of Technology, Yokohama, kanagawa, Japan. makoto.ohyama@meiji.com
authors: Makoto
authors: M
authors: Ohyama
authors: Yumiko
authors: Y
authors: Okada
authors: Masaaki
authors: M
authors: Takahashi
authors: Osamu
authors: O
authors: Sakanaka
authors: Maki
authors: M
authors: Matsumoto
authors: Kunio
authors: K
authors: Atsumi
mesh_terms: D000818:Animals; D000969:Antinematodal Agents / Q000737:chemistry* / Q000494:pharmacology*; D001197:Ascaridia / Q000187:drug effects*; D047630:Depsipeptides / Q000737:chemistry* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D015394:Molecular Structure; D010456:Peptides, Cyclic / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000969:Antinematodal Agents; D047630:Depsipeptides; C542265:PF1022E peptide, Rosellinia; D010456:Peptides, Cyclic; C075544:PF 1022A