Marchetti Chiara, Chan Daniel S H, Coyne Anthony G, Abell Chris
Department of Chemistry,University of Cambridge,Lensfield Road,Cambridge CB2 1EW,UK.
Parasitology. 2018 Feb;145(2):184-195. doi: 10.1017/S0031182016001876. Epub 2016 Nov 2.
Tuberculosis is an infectious disease associated with significant mortality and morbidity worldwide, particularly in developing countries. The rise of antibiotic resistance in Mycobacterium tuberculosis (Mtb) urgently demands the development of new drug leads to tackle resistant strains. Fragment-based methods have recently emerged at the forefront of pharmaceutical development as a means to generate more effective lead structures, via the identification of fragment molecules that form weak but high quality interactions with the target biomolecule and subsequent fragment optimization. This review highlights a number of novel inhibitors of Mtb targets that have been developed through fragment-based approaches in recent years.
结核病是一种在全球范围内导致重大死亡率和发病率的传染病，在发展中国家尤为如此。结核分枝杆菌（Mtb）中抗生素耐药性的增加迫切需要开发新的药物先导物来应对耐药菌株。基于片段的方法最近已成为药物开发的前沿手段，通过识别与目标生物分子形成弱但高质量相互作用的片段分子并随后进行片段优化，以生成更有效的先导结构。本文综述重点介绍了近年来通过基于片段的方法开发的一些新型结核分枝杆菌靶点抑制剂。
