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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
Published on: January 26, 2016
Synthesis and anthelmintic activity of cyclohexadepsipeptides with cyclohexylmethyl side chains
Peter Jeschke1, Achim Harder, Winfried Etzel
1Bayer CropScience AG, Research Insecticides, Chemistry Insecticides, Monheim am Rhein, Germany. peter.jeschke@bayercropscience.com <peter.jeschke@bayercropscience.com>
Abstract:
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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