Journal
MOLECULES
Volume 24, Issue 10, Pages -Publisher
MDPI
DOI: 10.3390/molecules24102021
Keywords
(3-benzyl-5-hydroxyphenyl)carbamate; Mycobacterium tuberculosis; antitubercular activity
Funding
- National Natural Science Foundation of China [21772240]
- Chinese Academy of Science [YJKYYQ20170036]
- Guangzhou Science Technology and Innovation Commission [201707010210, 201604020019]
- Science and Technology Innovation Leader of Guangdong Province [2016TX03R095]
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A series of 3-amino-5-benzylphenol derivatives were designed and synthesized. Among them, (3-benzyl-5-hydroxyphenyl)carbamates were found to exert good inhibitory activity against M. tuberculosis H37Ra, H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.625-6.25 g/mL). The privileged compounds 3i and 3l showed moderate cytotoxicity against cell line A549. Compound 3l also exhibited potent in vivo inhibitory activity on a mouse infection model via the oral administration. The results demonstrated 3-hydroxyphenylcarbamates as a class of new antitubercular agents with good potential.
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