Bedaquiline, also known as TMC207 and R207910, is a diarylquinoline anti-tuberculosis drug, which was discovered by a team led by Koen Andries at Janssen Pharmaceutica. Bedaquiline blocks the proton pump for ATP synthase of mycobacteria. ATP production is required for cellular energy production and its loss leads to cell death, even in dormant or nonreplicating mycobacteria.It is the first member of a new class of drugs called the diarylquinolines. Bedaquiline is bactericidal.
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Kong, De-Long; Huang, Ye; Ren, Lai-Yang; Feng, Wen-Hua. A highly efficient way to recycle inactive stereoisomers of Bedaquiline into two previous intermediates via base-catalyzed Csp3-Csp3 bond cleavage. Chinese Chemical Letters. Volume 26. Issue 6. Pages 790-792. Journal; Online Computer File. (2015).
Li, Jianqi; Liu, Yu; Bing, Shaochang; Wu, Xiabing; Zhou, Ainan; Huang, Lei; Jin, Renli; Wang, Jian; Jiang, Min; Wang, Lei. Method for preparing bedaquiline. Assignee China National Medicines Guorui Pharmaceutical Co., Ltd., Peop. Rep. China; Shanghai Institute of Pharmaceutical Industry. CN 105085395. (2015).