Martin, Liam T;
Daniel, Chris;
Guldberg-Allen, Marcus;
Navaratnarajah, Anushandan;
Anselmi, Silvia;
Burova, Tina-Maria D;
Willcocks, Sam;
... Bhakta, Sanjib; + view all
(2025)
Development of Carprofen analogues with activity against Mycobacterium tuberculosis.
Bioorganic & Medicinal Chemistry
, 127
, Article 118226. 10.1016/j.bmc.2025.118226.
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Abstract
Carprofen, a veterinary non-steroidal anti-inflammatory drug, has demonstrated bactericidal activity against Mycobacterium tuberculosis and the closely related model organism M. bovis BCG. Herein, we present the SAR-driven optimisation of three series of carbazole-based carprofen analogues for increased antimycobacterial potency and selectivity over the human monocyte-derived THP-1 cell line. An efficient synthetic route was employed to assemble a range of carprofen analogues which were then evaluated in whole-cell phenotypic assays to establish their activity against well-studied model organisms for M. tuberculosis. The most promising compound was further profiled against M. tuberculosis H37Rv, confirming the identification of a potent antitubercular carbazole with significantly enhanced therapeutic potential.
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