Buruli ulcer, a severe necrotizing skin disease caused by mycolactones, toxins secreted by Mycobacterium ulcerans, is one of the most neglected tropical diseases. Mycolactones are the first polyketides to be a human pathogen, and have immunosuppressive properties. Our objective is to provide several analogues and to develop the first structure-activity relationship (SAR) study of mycolactones aiming at better understanding their mode of action. A diverted total synthesis approach of mycolactones has been designed.This modular strategy allowed a rapid synthesis of a panel of analogs which have been evaluated. The cytopathicity results of the variants already obtained seems to be promising for the establishment of the first complete SAR study of this toxin.

First structure activity relationship of the mycolactones analogs

244th National Meeting (2012)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.