Cover Picture: Structural Simplification of Bedaquiline: the Discovery of 3‐(4‐(N, N‐Dimethylaminomethyl)phenyl)quinoline‐Derived Antitubercular Lead Compounds (ChemMedChem 2/2017). (20th January 2017)

• Record Type: Journal Article
• Authors: He, Chunxian; Preiss, Laura; Wang, Bin; Fu, Lei; Wen, Hui; Zhang, Xiang; Cui, Huaqing; Meier, Thomas; Yin, Dali
• Is Part Of: ChemMedChem. Volume 12:Number 2(2017)
• Page Start: 105
• Page End: 105
• Publication Date: 2017-01-20
• Subjects: ATP synthase -- bedaquiline -- multidrug resistance -- Mycobacterium tuberculosis -- pulmonary tuberculosis; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201600625
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract : 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. onpage 106 in Issue 2, 2017 (DOI:10.1002/cmdc.201600441 ). (The picture was drawn by Dr. Laura Preiss.)