Journal
CHEMMEDCHEM
Volume 14, Issue 3, Pages 349-358Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201800720
Keywords
antibacterial activity; Mycobacterium marinum; serine hydrolases; tuberculosis; beta-lactones
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Funding
- Centre National de la Recherche Scientifique (CNRS)
- Special Account for Research Grants of the National and Kapodistrian University of Athens (SARG/NKUA)
- Ministere de l'Enseignement Superieur de la Recherche et de l'Innovation, France
- Greek National Scholarship Foundation (IKY)
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In the quest for new antibacterial agents, a series of novel long- and medium-chain mono- and disubstituted beta-lactones was developed. Their activity against three pathogenic mycobacteria-M. abscessus, M. marinum, and M. tuberculosis-was assessed by the resazurin microtiter assay (REMA). Among the 16 beta-lactones synthesized, only 3-hexadecyloxetan-2-one (VM005) exhibited promising activity against M. abscessus, whereas most of the beta-lactones showed interesting activities against M. marinum, similar to that of the classical antibiotic, isoniazid. Regarding M. tuberculosis, six compounds were found to be active against this mycobacterium, with beta-lactone VM008 [trans-(Z)-3-(hexadec-7-en-1-yl)-4-propyloxetan-2-one] being the best growth inhibitor. The promising antibacterial activities of the best compounds in this series suggest that these molecules may serve as leads for the development of much more efficient antimycobacterial agents.
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