Glutathione-like tripeptides as inhibitors of glutathionyispermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group

被引：17

作者：

Amssons, K

Oza, SL

Ravaschino, E

Yamani, A

Lambeir, AM

Rajan, P

Bal, G

Rodriguez, JB

Fairlamb, AH

Augustyns, K

Haemers, A ^{[1
]}

机构：

[1] Univ Antwerp, Dept Med Chem, Antwerp, Belgium

[2] Univ Dundee, Dept Biochem, Dundee DD1 4HN, Scotland

[3] Univ Buenos Aires, Dept Quim Organ, FCEyN, Buenos Aires, DF, Argentina

[4] Univ Antwerp, Dept Biochem Med, Antwerp, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 18期

基金：

英国惠康基金;

关键词：

D O I：

10.1016/S0960-894X(02)00489-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Glutathionylspermidine synthetase/amidase (GspS) is an essential enzyme in the biosynthesis and turnover of trypanothione and represents an attractive target for the design of selective anti-parasitic drugs. We synthesised a series of analogues of glutathione (L-gamma-Glu-L-Leu-Gly-X) where the glycine carboxylic acid group (X) has been substituted for other acidic groups such as tetrazole, hydroxamic acid, acylsulphonamide and boronic acid. The boronic acid appears the most promising lead compound IC50 of 17.2 muM). (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2553 / 2556

页数：4

共 13 条

[1] Trypanothione as a target in the design of antitrypanosomal and antileishmanial agents [J].