Synthesis and anthelmintic activity of cyclohexadepsipeptides with cyclohexylmethyl side chains
| Autor: | Gerhard Thielking, Winfried Etzel, Peter Jeschke, Michael Schindler, Achim Harder |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Magnetic Resonance Spectroscopy
Stereochemistry Chemistry Pharmaceutical Clinical Biochemistry Pharmaceutical Science Sheep Diseases Biochemistry Chemical synthesis Peptides Cyclic Catalysis Mass Spectrometry Drug Discovery medicine Side chain Animals Humans Anthelmintic Molecular Biology Depsipeptide chemistry.chemical_classification Anthelmintics Sheep biology Chemistry Organic Chemistry Total synthesis biology.organism_classification Cyclic peptide Models Chemical Drug Design Molecular Medicine Haemonchus Enniatin Peptides Haemonchus contortus medicine.drug Hydrogen |
| Zdroj: | Bioorganicmedicinal chemistry letters. 17(13) |
| ISSN: | 0960-894X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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