Kim D H, Chung S J, Kim E J, Tian G R
Center for Biofunctional Molecules, Pohang University of Science and Technology, Korea.
Bioorg Med Chem Lett. 1998 Apr 7;8(7):859-64. doi: 10.1016/s0960-894x(98)00123-1.
alpha-Benzyl-2-oxo-1,3-oxazolidine-4-acetic acid (BOOA) having (alpha R,4S) and (alpha S,4R) configurations were designed and synthesized as a novel type of mechanism-based inactivators for carboxypeptidase A (CPA), and kinetic analysis demonstrated that they indeed inhibit the enzyme in a time-dependent manner with the second order inhibitory rate constants (kinact/KI) of 1.52 and 1.39 M-1 s-1 for (alpha S,R4)-BOOA and (alpha R,4S)-BOOA, respectively.
设计并合成了具有(αR,4S)和(αS,4R)构型的α-苄基-2-氧代-1,3-恶唑烷-4-乙酸(BOOA)，作为一种新型的基于机制的羧肽酶A(CPA)失活剂，动力学分析表明，它们确实以时间依赖性方式抑制该酶，(αS,4R)-BOOA和(αR,4S)-BOOA的二级抑制速率常数(kinact/KI)分别为1.52和1.39 M-1 s-1。
