Solid-phase synthesis of a focused library of trypanothione reductase inhibitors

被引：13

作者：

De Luca, S ^{[1
]}

Ulhaq, S ^{[1
]}

Dixon, MJ ^{[1
]}

Essex, J ^{[1
]}

Bradley, M ^{[1
]}

机构：

[1] Univ Southampton, Dept Chem, Southampton SO17 1BJ, Hants, England

来源：

TETRAHEDRON LETTERS | 2003年 / 44卷 / 15期

关键词：

D O I：

10.1016/S0040-4039(03)00438-6

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A focused library of inhibitors of the enzyme trypanothione reductase was prepared using solid-phase synthesis. The inhibitors were based on a previously identified, non-competitive, lead compound comprising of two Pmc (2,2,5,7,8-pentamethylchroman-6-sulfonyl) side-chain protected, N-capped arginine residues linked by a spermidine bridge. In total six protecting groups and four capping groups were used to generate a 24-membered library. All compounds bearing the 5-methoxyindole-3-acetic acid capping group were found to have good activity. The most potent inhibitor was observed to contain the Mtr (4-methoxy-2,3,6-trimethylbenzenesulphonyl) protecting group on the arginine residue, terminated with tryptophan as the capping group. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：3195 / 3197

页数：3

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