氨基磷酸酯和硫代磷酸酯二肽作为VanX的潜在抑制剂
Phosphonamidate and phosphothioate dipeptides as potential inhibitors of VanX.
作者信息
Yang K W, Brandt J J, Chatwood L L, Crowder M W
机构信息
Department of Chemistry and Biochemistry, Miami University, Oxford, OH 45056, USA.
出版信息
Bioorg Med Chem Lett. 2000 May 15;10(10):1085-7. doi: 10.1016/s0960-894x(00)00186-4.
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.
摘要
为了制备新型的VanX抑制剂，合成了N-[(1-氨基乙基)羟基膦酰基]-D-丙氨酸1和S-[(氨基乙基)羟基膦酰基]-硫代乙酸2，并将其作为VanX抑制剂进行评估。膦酰胺1被证明是VanX的部分竞争性抑制剂，其抑制常数Ki为36±3微摩尔，而硫代磷酸酯2则未显示出对VanX的抑制作用。
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