Synthesis and anthelmintic activity of cyclohexadepsipeptides with cyclohexylmethyl side chains.

Bioorg Med Chem Lett

Bayer CropScience AG, Research Insecticides, Chemistry Insecticides, Monheim am Rhein, Germany.

Published: July 2007

Cyclohexadepsipeptides (CHDPs) with cyclohexylmethyl side chains represent novel enniatins with in vivo activity against the parasitic nematode Haemonchus contortus Rudolphi in sheep. It was found that the replacement of benzylic by cyclohexylmethyl side chains on the enniatin skeleton can increase anthelmintic efficacy. Here we report on a simple total synthesis of the precursors for this type of CHDPs and an efficient chemical transformation of the benzylic into the corresponding cyclohexylmethyl side chains.

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Source
http://dx.doi.org/10.1016/j.bmcl.2007.04.037DOI Listing

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