Synthesis and activity of the glutathione analogue gamma-(L-gamma-oxaglutamyl)-L-cysteinyl-glycine

被引：15

作者：

Calcagni, A

Dupre, S

Lucente, G

Luisi, G

Pinnen, F

Rossi, D

Spirito, A

机构：

[1] UNIV ROMA LA SAPIENZA,DIPARTIMENTO SCI BIOCHIM,ROME,ITALY

[2] CATANIA UNIV,IST CHIM FARMACEUT,CATANIA,ITALY

来源：

ARCHIV DER PHARMAZIE | 1996年 / 329卷 / 11期

关键词：

enzyme inhibitors; gamma-glutamyltransferase; glutathione analogues; L-gamma-oxaglutamic acid;

D O I：

10.1002/ardp.19963291105

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An efficient synthesis of the backbone modified glutathione analogue gamma-(L-gamma-oxaglutamyl)-L-cysteinyl-glycine (7), characterized by the presence of an urethane O-CO-NH linkage replacing the gamma-glutamylic CH2CO-NH fragment is described. The new analogue has been fully characterized by H-1- and C-13-NMR and FAB-MS. Compound 7 was tested for inhibition of gamma-glutamyltransferase asl activity and was found to be a non-competitive inhibitor of hog kidney gamma-glutamyltransferase (EC 2.3.2.2).

引用

页码：498 / 502

页数：5

共 22 条

[1] AN IMPROVED METHOD FOR HETERONUCLEAR CHEMICAL-SHIFT CORRELATION BY TWO-DIMENSIONAL NMR [J].