Synthesis of novel [1,2]-diamines with antituberculosis activity.
Guided by the metabolism information of SQ109, derivatives with substituted geranylamine moiety or substituted admantane ring of SQ109 were synthesized and evaluated as antituberculosis agents. Among all tested compounds, compound 11c showed the most potent antituberculosis activity with MIC value of 0.3 microM against Mycobacterium tuberculosis H37Rv.
Meng
Qingyi
Q
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Luo
Huibing
H
Chen
Yilang
Y
Wang
Tiancai
T
Yao
Qizheng
Q
D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003959:Diamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy
D000995:Antitubercular Agents; D003959:Diamines