Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy
oleh: Ya-Juan Cheng, Zhi-Yong Liu, Hua-Ju Liang, Cui-Ting Fang, Niu-Niu Zhang, Tian-Yu Zhang, Ming Yan
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2019-05-01 |
Deskripsi
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 <i>M. tuberculosis</i> H37Ra, H37Rv and clinically isolated multidrug-resistant <i>M. tuberculosis</i> strains (MIC = 0.625−6.25 μg/mL). The privileged compounds <b>3i</b> and <b>3l</b> showed moderate cytotoxicity against cell line A549. Compound <b>3l</b> 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.