Synthetic approaches towards bedaquiline and its derivatives.

Bioorg Med Chem Lett

School of Chemical Sciences, The University of Auckland, Symonds Street, Auckland 1010, New Zealand; Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Symonds Street, Auckland 1010, New Zealand. Electronic address:

Published: June 2020

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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http://dx.doi.org/10.1016/j.bmcl.2020.127172DOI Listing

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