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.