Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis |
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| Authors: | Yasuhiro Horita Takemasa Takii Taku Chiba Ryuji Kuroishi Yasuhiro Maeda Yukihisa Kurono Emi Inagaki Kenji Nishimura Yoshifumi Yamamoto Chiyoji Abe Masami Mori Kikuo Onozaki |
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| Affiliation: | aDepartment of Molecular Health Sciences, Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, Japan;bCollege of Pharmacy, Kinjo Gakuin University, Nagoya, Japan;cDepartment of Hospital Pharmacy, Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, Japan;dResearch Institute of Tuberculosis, Japan Anti-Tuberculosis Association, Kiyose, Tokyo, Japan |
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| Abstract: | A series of sugar derivatives (1–13) were synthesized and evaluated for antibacterial activity against Mycobacterium tuberculosis (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-β-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. |
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| Keywords: | Carbohydrate Tuberculosis Antibacterial activity |
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