Authors: Anish Parmar, Abhishek Iyer, Charlotte S. Vincent, Dorien Van Lysebetten, Stephen H. Prior, Annemieke Madder, Edward J. Taylor, Ishwar Singh
Summary: The discovery of the new antibiotic teixobactin has been timely in the race for unearthing novel antibiotics wherein the emergence of drug resistant bacteria poses a serious threat worldwide. Herein, we present the total syntheses and biological activities of two teixobactin analogues. This approach is simple, efficient and has several advantages: it uses commercially available building blocks (except AllocHN-D-Thr-OH), has a single purification step and a good recovery (22%). By using this approach we have synthesised two teixobactin analogues and established that the D-amino acids are critical for the antimicrobial activity of these analogues. With continuing high expectations from teixobactin, this work can be regarded as a stepping stone towards an in depth study of teixobactin, its analogues and the quest for synthesising similar molecules.
Source:
Chemical Communications; 2016, 52 (36): 6060