Design and synthesis of 6-(6-D-ribitylamino-2,4-dihydroxypyrimidin-5-yl)-1-hexylphosphonic acid, a potent inhibitor of lumazine synthase

被引:18
作者
Cushman, M [1 ]
Mihalic, JT
Kis, K
Bacher, A
机构
[1] Purdue Univ, Sch Pharm & Pharmacal Sci, Dept Med Chem & Mol Pharmacol, W Lafayette, IN 47907 USA
[2] Tech Univ Munich, Lehrstuhl Organ Chem & Biochem, D-85747 Garching, Germany
关键词
D O I
10.1016/S0960-894X(98)00687-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A novel inhibitor of lumazine synthase, the penulrimate enzyme in the biosynthesis of riboflavin, has been synthesized. The inhibitor was designed by computer graphics molecular modeling using a hypothetical structure of the enzyme-inhibitor complex. The new compound is relatively potent when compared with the known inhibitors, and displays a K-I of 109 mu M. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:39 / 42
页数:4
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