Design,synthesis and antimycobacterial activity of novel nitrobenzamide derivatives

被引:0
|
作者
Hongjian Wang [1 ]
Kai Lv [1 ]
Xiaoning Li [1 ]
Bo Wang [1 ]
Apeng Wang [1 ]
Zeyu Tao [1 ]
Yunhe Geng [1 ]
Bin Wang [2 ]
Menghao Huang [3 ]
Mingliang Liu [1 ]
Huiyuan Guo [1 ]
Yu Lu [2 ]
机构
[1] Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College
[2] Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute,Beijing Chest Hospital, Capital Medical University
[3] Division of Gastroenterology and Hepatology, Department of Medicine, Indiana University School of Medicine
关键词
Nitrobenzamides; Synthesis; Antimycobacterial activity; Tuberculosis;
D O I
暂无
中图分类号
TQ465 [抗菌素制造];
学科分类号
100705 ;
摘要
We report herein the design and synthesis of a series of novel nitrobenzamide derivatives. Results reveal that many of them display considerable in vitro antitubercular activity. Four N-benzyl or N- (pyridine-2-yl)methyl 3,5-dinitrobenzamides A6, All, Cl and C4 have not only the same excellent MIC values of<0.016 μg/mL against both drug-sensitive MTB strain H37 Rv and two drug-resistant clinical isolates as PBTZ169 and the lead 1, but also acceptable safety indices (SI > 1500), opening a new direction for further development.
引用
收藏
页码:413 / 416
页数:4
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