Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
Horita Y, Takii T, Chiba T, Kuroishi R, Maeda Y, Kurono Y, Inagaki E, Nishimura K, Yamamoto Y, Abe C, Mori M, Onozaki K.
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.