Structure-Activity Relationship of Anthelmintic Cyclooctadepsipeptides | Zendy

Makoto Ohyama | Zendy; Yumiko Okada | Zendy; Masaaki Takahashi | Zendy; Osamu Sakanaka | Zendy; Maki Matsumoto | Zendy; Kunio Atsumi | Zendy

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Structure-Activity Relationship of Anthelmintic Cyclooctadepsipeptides

Author(s) -

Makoto Ohyama,

Yumiko Okada,

Masaaki Takahashi,

Osamu Sakanaka,

Maki Matsumoto,

Kunio Atsumi

Publication year - 2011

Publication title -

bioscience biotechnology and biochemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.509

H-Index - 116

eISSN - 1347-6947

pISSN - 0916-8451

DOI - 10.1271/bbb.110129

Subject(s) - anthelmintic , moiety , lipophilicity , ascaridia galli , nematode , in vivo , stereochemistry , structure–activity relationship , chemistry , pharmacology , helminths , biology , in vitro , biochemistry , ecology , zoology , microbiology and biotechnology

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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