Eur J Med Chem 2021 May 1;221:113488. Epub 2021 May 1.
National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, PR China; Laboratoire de Méthodologie, Synthèse et Molécules Thérapeutiques (ICMMO), UMR 8182, CNRS, Université Paris-Saclay, Bât 410, Facultédes Sciences D'Orsay, Orsay, 291405, France; State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, 15 Yuchai Road, Guilin, 541004, PR China. Electronic address:
Naturally occurring cyclic antimicrobial peptides (AMPs) such as tyrocidine A (Tyrc A) and gramicidin S (GS) are appealing targets for the development of novel antibiotics. However, their therapeutic potentials are limited by undesired hemolytic activity and relatively poor activity against Gram-negative bacteria. Inspired by polycationic lipopeptide polymyxin B (PMB), the so called 'last-resort' antibiotic for the treatment of infections caused by multidrug-resistant Gram-negative bacteria, we synthesized and biologically evaluated a series of polycationic analogues derived from Tyrc A. Read More