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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.
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页码:413 / 416
页数:4
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