ArticleNature chemistry2025
Discovery of a fluorinated macrobicyclic antibiotic through chemical synthesis.
Article in Nature chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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Who cites it
4 citing papers in PubMed.
- A multi-stage computational pipeline andRSC advances · 2026Article
- Article
- Practical Synthesis of Oxepanoprolines.Organic process research & development · 2025Article
- Practical Synthesis of Macrobicyclic Thiolincosamines.Journal of the American Chemical Society · 2024Article
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Authors and funding
9 authors.
Funding
Abstract
The emergence of bacterial antimicrobial resistance threatens to undermine the utility of antibiotic therapy in medicine. This threat can be addressed, in part, by reinventing existing antibiotic classes using chemical synthesis. Here we present the discovery of BT-33, a fluorinated macrobicyclic oxepanoprolinamide antibiotic with broad-spectrum activity against multidrug-resistant bacterial pathogens. Structure-activity relationships within the macrobicyclic substructure reveal structural features that are essential to the enhanced potency of BT-33 as well as its increased metabolic stability relative to its predecessors clindamycin, iboxamycin and cresomycin. Using X-ray crystallography, we determine the structure of BT-33 in complex with the bacterial ribosome revealing that its fluorine atom makes an additional van der Waals contact with nucleobase G2505. Through variable-temperature
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Registered trials
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