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Phosphonamidate and phosphothioate dipeptides as potential inhibitors of VanX
K W Yang1, J J Brandt, L L Chatwood
1Department of Chemistry and Biochemistry, Miami University, Oxford, OH 45056, USA.
Bioorganic & Medicinal Chemistry Letters
|June 8, 2000
Abstract:
In an effort to prepare novel inhibitors of VanX, N-[(1-aminoethyl)hydroxyphosphinyl]-D-alanine 1 and S-[(aminoethyl)hydroxyphosphinyl]-thiolacetic acid 2 were synthesized and evaluated as inhibitors of VanX. Phosphonamidate 1 was shown to be a partial competitive inhibitor of VanX with a Ki of 36+/-3 microM, and phosphothioate 2 was shown not to inhibit VanX.