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© Research
Publication : Chemistry (Weinheim an der Bergstrasse, Germany)

A diverted total synthesis of mycolactone analogues: an insight into Buruli ulcer toxins

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Chemistry (Weinheim an der Bergstrasse, Germany) - 30 Nov 2011

Chany AC, Casarotto V, Schmitt M, Tarnus C, Guenin-Macé L, Demangel C, Mirguet O, Eustache J, Blanchard N

Link to Pubmed [PMID] – 22127975

Chemistry 2011 Dec;17(51):14413-9

Mycolactones are complex macrolides responsible for a severe necrotizing skin disease called Buruli ulcer. Deciphering their functional interactions is of fundamental importance for the understanding, and ultimately, the control of this devastating mycobacterial infection. We report herein a diverted total synthesis approach of mycolactones analogues and provide the first insights into their structure-activity relationship based on cytopathic assays on L929 fibroblasts. The lowest concentration inducing a cytopathic effect was determined for selected analogues, allowing a clear picture to emerge by comparison with the natural toxins.

http://www.ncbi.nlm.nih.gov/pubmed/22127975