Structure-activity relationship of anthelmintic cyclooctadepsipeptides |
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Authors: | Ohyama Makoto Okada Yumiko Takahashi Masaaki Sakanaka Osamu Matsumoto Maki Atsumi Kunio |
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Affiliation: | Department of Electronic Chemistry, Interdisciplinary Graduate School of Science and Engineering, Tokyo Institute of Technology, Yokohama, kanagawa, Japan. makoto.ohyama@meiji.com |
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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. |
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