Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy.
Ya-Juan ChengZhi-Yong LiuHua-Ju LiangCui-Ting FangNiu-Niu ZhangTian-Yu ZhangMing YanPublished in: Molecules (Basel, Switzerland) (2019)
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 μg/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.
Keyphrases
- mycobacterium tuberculosis
- multidrug resistant
- pulmonary tuberculosis
- hiv aids
- escherichia coli
- small molecule
- rheumatoid arthritis
- anti inflammatory
- drug resistant
- high intensity
- acinetobacter baumannii
- gram negative
- klebsiella pneumoniae
- emergency department
- disease activity
- human health
- adverse drug
- ankylosing spondylitis
- cystic fibrosis
- climate change
- single cell