Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
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.
Horita
Yasuhiro
Y
Department of Molecular Health Sciences, Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, Japan.
Takii
Takemasa
T
Chiba
Taku
T
Kuroishi
Ryuji
R
Maeda
Yasuhiro
Y
Kurono
Yukihisa
Y
Inagaki
Emi
E
Nishimura
Kenji
K
Yamamoto
Yoshifumi
Y
Abe
Chiyoji
C
Mori
Masami
M
Onozaki
Kikuo
K
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002241:Carbohydrates; D002626:Chemistry, Pharmaceutical; D015195:Drug Design; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000737:chemistry
D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D002241:Carbohydrates; D013440:Sulfides