Synthetic approaches towards bedaquiline and its derivatives |
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| Institution: | 1. School of Chemical Sciences, The University of Auckland, Symonds Street, Auckland 1010, New Zealand;2. Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Symonds Street, Auckland 1010, New Zealand;3. Global Alliance for TB Drug Development, 40 Wall Street, New York, NY 10005, USA;1. Cedilla Therapeutics, 38 Sidney Street, Cambridge, MA 02139, USA;2. Research Platforms, Sanofi, 13 Quai Jules Guesde, Vitry-sur-Seine 94400, France;1. Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute BS, 10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India;2. Microbiology Division, CSIR-Central Drug Research Institute BS 10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India;3. Academiy of Scientific and Innovative Research, New Delhi 110001, India;1. Auckland Cancer Society Research Centre, School of Medical Sciences, and Maurice Wilkins Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand;2. Maurice Wilkins Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand;3. Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, USA;4. Global Alliance for TB Drug Development, 40 Wall St, New York, NY 10005, USA;1. National Engineering Research Center for the Emergency Drug, Beijing Institute of Pharmacology and Toxicology, Taiping Road 27, Beijing 100850, PR China;2. Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University, Beijing, PR China |
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| Abstract: | Bedaquiline is a diarylquinoline drug that demonstrates potent and selective inhibition of mycobacterial ATP synthase, and is clinically administered for the treatment of multi-drug resistant tuberculosis. Due to its excellent activity and novel mechanism of action, bedaquiline has been the focus of a number of synthetic studies. This review will discuss these synthetic approaches, as well as the synthesis and bioactivity of the numerous derivatives and molecular probes inspired by bedaquiline. |
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| Keywords: | Bedaquiline Tuberculosis Diarylquinolines Stereoselective synthesis SAR |
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