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Synthesis of Long-Chain β-Lactones and Their Antibacterial Activities against Pathogenic Mycobacteria

Abstract : In the quest for new antibacterial agents, a series of novel long and medium chain mono-and disubstituted β-lactones has been developed. Their respective antibacterial activity using the resazurin microtiter assay (REMA) was further assessed against three pathogenic mycobacteria: M. abscessus, M. marinum and M. tuberculosis. Among the 16 β-lactones synthesized, only VM005 exhibited promising activity against M. abscessus; while most of the β-lactones showed interesting activities against M. marinum, similar to those of classical antibiotic, isoniazid. Regarding M. tuberculosis, 6 compounds were found active against this mycobacterium, with β-lactone VM008 being the best growth inhibitor. The promising antibacterial activities of the best compounds suggest that these molecules may serve as potential leads for the development of much more efficient anti-mycobacterial agents.
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Submitted on : Wednesday, January 29, 2020 - 5:52:38 PM
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Pierre Santucci, Christina Dedaki, Alexandros Athanasoulis, Laura Gallorini, Anaïs Munoz, et al.. Synthesis of Long-Chain β-Lactones and Their Antibacterial Activities against Pathogenic Mycobacteria. ChemMedChem, Wiley-VCH Verlag, 2019, 14 (3), pp.349-358. ⟨10.1002/cmdc.201800720⟩. ⟨hal-01990100⟩

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