title: Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
abstract: 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.
authors.affiliation: Department of Molecular Health Sciences, Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, Japan.
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Horita
authors.forename: Takemasa
authors.initials: T
authors.lastname: Takii
authors.forename: Taku
authors.initials: T
authors.lastname: Chiba
authors.forename: Ryuji
authors.initials: R
authors.lastname: Kuroishi
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Maeda
authors.forename: Yukihisa
authors.initials: Y
authors.lastname: Kurono
authors.forename: Emi
authors.initials: E
authors.lastname: Inagaki
authors.forename: Kenji
authors.initials: K
authors.lastname: Nishimura
authors.forename: Yoshifumi
authors.initials: Y
authors.lastname: Yamamoto
authors.forename: Chiyoji
authors.initials: C
authors.lastname: Abe
authors.forename: Masami
authors.initials: M
authors.lastname: Mori
authors.forename: Kikuo
authors.initials: K
authors.lastname: Onozaki
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D002241:Carbohydrates; D013440:Sulfides