Cover Picture: Structural Simplification of Bedaquiline: the Discovery of 3-(4-(N,N-Dimethylaminomethyl)phenyl)quinoline-Derived Antitubercular Lead Compounds (ChemMedChem 2/2017)

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• 作者：Dr. Chunxian He ; Dr. Laura Preiss ; Bin Wang ; Lei Fu ; Hui Wen ; Xiang Zhang ; Dr. Huaqing Cui ; Prof. Thomas Meier and Prof. Dali Yin
• 刊名：ChemMedChem
• 出版年：2017
• 出版时间：January 20, 2017
• 年：2017
• 卷：12
• 期：2
• 页码：105
• 全文大小：496K
• ISSN：1860-7187

文摘

The front cover picture shows a molecular model of a bacterial rotary ATP synthase, which is targeted and inhibited by the novel antituberculosis (TB) drug Bedaquiline (Sirturo®), the first anti-TB antibiotic compound in 40 years. Bedaquiline synthesis is expensive, mainly due to two chiral centers within the molecule. Using a fragment based synthesis approach He, Preiss et al. present an economical way of producing Bedaquiline derivatives with no chiral centers that still maintain antitubercular activity against Mycobacterium tuberculosis. More information can be found in the Full Paper by Huaqing Cui, Thomas Meier, Dali Yin et al. on page 106 in Issue 2, 2017 (DOI: 10.1002/cmdc.201600441). (The picture was drawn by Dr. Laura Preiss.)