Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents.
A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by (1)H NMR, (13)C NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20-100 mg/L. Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC(50) against THP-1 cells greater than 100 mg/L.
State-Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center(Tianjin), Nankai University, Tianjin 300071, China.
Li
L
Pan
Ying
Y
Jiang
Zhen
Z
Liu
Xing-Hai
XH
Liu
Zhuo
Z
Liu
Gang
G
Wang
Zheng-Ming
ZM
Li
Di
D
Wang
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009000:Monocytes / Q000166:cytology / Q000187:drug effects*; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013453:Sulfonylurea Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D014376:Tuberculosis / Q000188:drug therapy*
D000995:Antitubercular Agents; D013453:Sulfonylurea Compounds