Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis

被引:26
作者
Horita, Yasuhiro [1 ]
Takii, Takemasa [1 ]
Chiba, Taku [2 ]
Kuroishi, Ryuji [1 ]
Maeda, Yasuhiro [3 ]
Kurono, Yukihisa [3 ]
Inagaki, Emi [1 ]
Nishimura, Kenji [1 ]
Yamamoto, Yoshifumi [1 ]
Abe, Chiyoji [4 ]
Mori, Masami [2 ]
Onozaki, Kikuo [1 ]
机构
[1] Nagoya City Univ, Grad Sch Pharmaceut Sci, Dept Mol Hlth Sci, Nagoya, Aichi, Japan
[2] Kinjo Gakuin Univ, Coll Pharm, Nagoya, Aichi, Japan
[3] Nagoya City Univ, Grad Sch Pharmaceut Sci, Dept Hosp Pharm, Nagoya, Aichi, Japan
[4] Japan AntiTB Assoc, Res Inst TB, Tokyo, Japan
关键词
Carbohydrate; Tuberculosis; Antibacterial activity;
D O I
10.1016/j.bmcl.2009.09.095
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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-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. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6313 / 6316
页数:4
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