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.
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.
基金
supported by the National Mega-project for Innovative Drugs(Nos.2015ZX09102007-008,2015ZX09102007015,2015ZX0 9304006-016,2018ZX09721001-004-007, 2018ZX09711001-007-002)
CAMS Initiative for Innovative Medicine(No.2016-I2M-1-010)
CAMS Innovation Fund for Medical Science(Nos.CAMS-2016-I2M-1-010,CAMS-2017-I2M-1-011)
PUMC Youth Fund (No. 2017350011)
