The macrocyclic antibiotic mangrolide A has been described to exhibit potent activity against a number of clinically important Gram‐negative pathogens. Reported is the first enantioselective total synthesis of mangrolide A and derivatives. Salient features of this synthesis include a highly convergent macrocycle preparation, stereoselective synthesis of the disaccharide moiety, and two β‐selective glycosylations. The synthesis of mangrolide A and its analogues enabled the re‐examination of its activity against bacterial pathogens, and only minimal activity was observed.

+More

macrocycle preparation stereoselective

Hiromu Hattori , Joel Roesslein , Dr. Patrick Caspers , Dr. Katja Zerbe , Dr. Hideki Miyatake‐Ondozabal , Dr. Daniel Ritz , Dr. Georg Rueedi , Prof. Dr. Karl Gademann,.Total Synthesis and Biological Evaluation of the Glycosylated Macrocyclic Antibiotic Mangrolide A. 57 (57),11020-11024.

Hiromu Hattori , Joel Roesslein , Dr. Patrick Caspers , Dr. Katja Zerbe , Dr. Hideki Miyatake‐Ondozabal , Dr. Daniel Ritz , Dr. Georg Rueedi , Prof. Dr. Karl Gademann,"Total Synthesis and Biological Evaluation of the Glycosylated Macrocyclic Antibiotic Mangrolide A" 57

Hiromu Hattori , Joel Roesslein , Dr. Patrick Caspers , Dr. Katja Zerbe , Dr. Hideki Miyatake‐Ondozabal , Dr. Daniel Ritz , Dr. Georg Rueedi , Prof. Dr. Karl Gademann,"Total Synthesis and Biological Evaluation of the Glycosylated Macrocyclic Antibiotic Mangrolide A"