Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils
Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils
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DOI：
10.1016/j.bmc.2007.03.012
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发表时间：
2007-06-01
影响因子：
3.5
通讯作者：
Potter, Philip M.
中科院分区：
文献类型：
--
作者：
Hicks, Latorya D.;Hyatt, Janice L.;Potter, Philip M.
我们已经合成并评估了对称的氟代苯偶姻和氟代苯偶酰抑制哺乳动物羧酸酯酶（CE）的能力。后者中的大多数是CE的优异抑制剂，然而出乎意料的是，氟苯偶姻是非常好的酶抑制剂。与羟基碳原子上的电荷、羰基氧和Hammett常数正相关，用于用氟苯偶姻导出的Ki值。(c)2007爱思唯尔有限公司版权所有。
We have synthesized and assessed the ability of symmetrical fluorobenzoins and fluorobenzils to inhibit mammalian carboxylesterases (CE). The majority of the latter were excellent inhibitors of CEs however unexpectedly, the fluorobenzoins were very good enzyme inhibitors. Positive correlations were seen with the charge on the hydroxyl carbon atom, the carbonyl oxygen, and the Hammett constants for the derived K-i values with the fluorobenzoins. (c) 2007 Elsevier Ltd. All rights reserved.