EVALUATION OF PHOSPHORUS-CONTAINING INHIBITORS OF GAMMA-GLUTAMYL HYDROLASE

Authors
RODRIGUEZ CE HOLMES HM MLODNOSKY KL LAM VQ BERKMAN CE
Citation
Ce. Rodriguez et al., EVALUATION OF PHOSPHORUS-CONTAINING INHIBITORS OF GAMMA-GLUTAMYL HYDROLASE, Bioorganic & medicinal chemistry letters, 8(12), 1998, pp. 1521-1524
Citations number
12
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
12
Year of publication
1998
Pages
1521 - 1524
Database
ISI
SICI code
0960-894X(1998)8:12<1521:EOPIOG>2.0.ZU;2-U
Abstract
Several putative, phosphorus-containing inhibitors of gamma-glutamyl h ydrolase were synthesized and evaluated for inhibitory activity. The p hosphonamidoic acids were shown to be weak competitive inhibitors whil e both a phosphoramidate diester and a phosphonamidate ester were show n to be potent time-dependent inactivators, presumably through irrever sible phosphorylation of an active site nucleophile. (C) 1998 Elsevier Science Ltd. All rights reserved.