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Issue 40, 2016
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New synthetic approaches towards analogues of bedaquiline

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Multi-drug resistant tuberculosis (MDR-TB) is of growing global concern and threatens to undermine increasing efforts to control the worldwide spread of tuberculosis (TB). Bedaquiline has recently emerged as a new drug developed to specifically treat MDR-TB. Despite being highly effective as a result of its unique mode of action, bedaquiline has been associated with significant toxicities and as such, safety concerns are limiting its clinical use. In order to access pharmaceutical agents that exhibit an improved safety profile for the treatment of MDR-TB, new synthetic pathways to facilitate the preparation of bedaquiline and analogues thereof have been discovered.

Graphical abstract: New synthetic approaches towards analogues of bedaquiline

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The article was received on 29 Aug 2016, accepted on 13 Sep 2016 and first published on 13 Sep 2016

Article type: Paper
DOI: 10.1039/C6OB01893A
Org. Biomol. Chem., 2016,14, 9622-9628

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    New synthetic approaches towards analogues of bedaquiline

    D. L. Priebbenow, L. Barbaro and J. B. Baell, Org. Biomol. Chem., 2016, 14, 9622
    DOI: 10.1039/C6OB01893A

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