AI Article Synopsis
- Despite its effectiveness, bedaquiline's clinical use is limited due to safety issues.
- Researchers investigated changes in the quinoline ring of bedaquiline to create safer variants.
- They found that substituting the quinoline structure with pyridine still retained anti-tubercular activity, leading to new opportunities for developing better treatments.
Article 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.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8221263 | PMC |
| http://dx.doi.org/10.1039/d1md00063b | DOI Listing |
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