Synthesis and evaluation of thymidine-5′-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase

被引：53
|
作者：
Vanheusden, V
Munier-Lehmann, H
Pochet, S
Herdewijn, P
Van Calenbergh, S
机构：
[1] Univ Ghent, Lab Med Chem FFW, B-9000 Ghent, Belgium
[2] Inst Pasteur, Lab Chim Struct Macromol, F-75724 Paris 15, France
[3] Inst Pasteur, Unite Organ, F-75724 Paris 15, France
[4] Katholieke Univ Leuven, Rega Inst, Med Chem Lab, B-3000 Louvain, Belgium
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 19期
关键词：
D O I：
10.1016/S0960-894X(02)00551-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A number of 2'- and 3'-modified thymidine 5'-O-monophosphate analogues were synthesized as potential leads for new anti-mycobacterial drugs. Evaluation of their affinity for Mycobacterium tuberculosis thymidine monophosphate kinase showed that a 2'-halogeno substituent and a 3'-azido function are the most favorable leads for further development of potent inhibitors of this enzyme. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2695 / 2698
页数：4
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