1. Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy
- Author
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Ya-Juan Cheng, Tianyu Zhang, Ming Yan, Hua-Ju Liang, Zhiyong Liu, Cuiting Fang, and Niu-Niu Zhang
- Subjects
Tuberculosis ,Antitubercular Agents ,Pharmaceutical Science ,antitubercular activity ,Microbial Sensitivity Tests ,Pharmacology ,Inhibitory postsynaptic potential ,complex mixtures ,01 natural sciences ,Article ,Analytical Chemistry ,Mycobacterium tuberculosis ,lcsh:QD241-441 ,03 medical and health sciences ,lcsh:Organic chemistry ,Oral administration ,In vivo ,Drug Resistance, Multiple, Bacterial ,Drug Discovery ,medicine ,Animals ,Humans ,heterocyclic compounds ,Physical and Theoretical Chemistry ,Cytotoxicity ,0303 health sciences ,(3-benzyl-5-hydroxyphenyl)carbamate ,Cell Death ,biology ,030306 microbiology ,Chemistry ,organic chemicals ,Organic Chemistry ,medicine.disease ,biology.organism_classification ,In vitro ,0104 chemical sciences ,Disease Models, Animal ,010404 medicinal & biomolecular chemistry ,Treatment Outcome ,A549 Cells ,Chemistry (miscellaneous) ,Cell culture ,Molecular Medicine ,Carbamates - Abstract
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&ndash, 6.25 &mu, 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. more...
- Published
- 2019