Phosphonamidate and phosphothioate dipeptides as potential inhibitors of VanX

Authors
Yang, KW Brandt, JJ Chatwood, LL Crowder, MW
Citation
Kw. Yang et al., Phosphonamidate and phosphothioate dipeptides as potential inhibitors of VanX, BIOORG MED, 10(10), 2000, pp. 1085-1087
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
10
Year of publication
2000
Pages
1085 - 1087
Database
ISI
SICI code
0960-894X(20000515)10:10<1085:PAPDAP>2.0.ZU;2-C
Abstract
In an effort to prepare novel inhibitors of VanX, N-[(1-aminoethyl)hydroxyp hosphinyl]-D-alanine 1 and S-[(aminoethyl)hydroxyphosphinyl]-thiolacetic ac id 2 were synthesized and evaluated as inhibitors of VanX. Phosphonamidate 1 was shown to be a partial competitive inhibitor of VanX with a K-i of 36/-3 mu M, and phosphothioate 2 was shown not to inhibit VanX. (C) 2000 Else vier Science Ltd. All rights reserved.