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. 2012 Aug:54:582-90.
doi: 10.1016/j.ejmech.2012.06.009. Epub 2012 Jun 15.

Synthesis and anthelmintic activity of osthol analogs against Dactylogyrus intermedius in goldfish

Guang-Lu Liu  1 , Bing Hao, Shao-Peng Liu, Gao-Xue Wang
Affiliations

Synthesis and anthelmintic activity of osthol analogs against Dactylogyrus intermedius in goldfish

Guang-Lu Liu et al. Eur J Med Chem. 2012 Aug.

Abstract

In an attempt to develop novel anthelmintic agents, our previously isolated osthol was used as lead structures for further optimization. In our research, a series of coumarin analogs, prepared from 7-hydroxy coumarin or 7-hydroxy-4-methyl coumarin, have been evaluated for their anthelmintic activities. In all of the compounds, 6 and 7 were first synthesized, and their structures were identified based on NMR and MS values. Among the candidates, 8-allyl-7-allyloxycoumarin showed better anthelmintic activity than other compounds against Dactylogyrus infestation with EC(50) value of 1.81 mg/L. The quantitative structure-activity relationship (QSAR) of 16 osthol analogs with anthelmintic activity expressed as pEC(50) and toxicity to goldfish expressed pLC(50), such results can offer useful theoretical references for future experimental works.

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