Department of Molecular Health Sciences, Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, Japan.
Bioorg Med Chem Lett. 2009 Nov 15;19(22):6313-6. doi: 10.1016/j.bmcl.2009.09.095. Epub 2009 Sep 27.
A series of sugar derivatives (1-13) were synthesized and evaluated for antibacterial activity against Mycobacteriumtuberculosis (MTB), especially multi-drug resistant (MDR) MTB, and the structure-activity relationships of these compounds were studied. The results showed that the compound OCT313 (2-acetamido-2deoxy-beta-D-glucopyranosyl N,N-dimethyldithiocarbamate) (4) exhibited significant in vitro bactericidal activity, and that the dithiocarbamate group at C-1 position of the glucopyranoside ring was requisite for the antibacterial activity.
一系列糖衍生物(1-13)被合成并评估了对结核分枝杆菌(MTB),特别是耐多药 MTB 的抗菌活性,并且研究了这些化合物的构效关系。结果表明,化合物 OCT313(2-乙酰氨基-2-脱氧-β-D-吡喃葡萄糖基 N,N-二甲基二硫代氨基甲酸盐)(4)表现出显著的体外杀菌活性,并且吡喃葡萄糖环 C-1 位的二硫代氨基甲酸盐基团是抗菌活性所必需的。