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Synthesis and evaluation of pyridine-derived bedaquiline analogues containing modifications at the A-ring subunit.
- Source :
-
RSC medicinal chemistry [RSC Med Chem] 2021 May 07; Vol. 12 (6), pp. 943-959. Date of Electronic Publication: 2021 May 07 (Print Publication: 2021). - Publication Year :
- 2021
-
Abstract
- Despite promising efficacy, the clinical use of the anti-tubercular therapeutic bedaquiline has been restricted due to safety concerns. To date, limited SAR studies have focused on the quinoline ring (A-ring), and as such, we set out to explore modifications within this region in an attempt to discover new bedaquiline variants with an improved safety profile. We herein report the development of unique synthetic strategies that facilitated access to novel bedaquiline analogues leading to the discovery that anti-tubercular activity could be retained following replacement of the quinoline motif with pyridine heterocycles. This discovery is anticipated to open up multiple new avenues for exploration in the design of improved anti-tubercular therapeutics.<br />Competing Interests: There are no conflicts to declare.<br /> (This journal is © The Royal Society of Chemistry.)
Details
- Language :
- English
- ISSN :
- 2632-8682
- Volume :
- 12
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- RSC medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 34223160
- Full Text :
- https://doi.org/10.1039/d1md00063b