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新型氟代苯偶姻和氟代苯偶酰对哺乳动物羧酸酯酶抑制作用的分析

Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils.

作者信息

Hicks Latorya D, Hyatt Janice L, Moak Teri, Edwards Carol C, Tsurkan Lyudmila, Wierdl Monika, Ferreira Antonio M, Wadkins Randy M, Potter Philip M

机构信息

Department of Molecular Pharmacology, St. Jude Children's Research Hospital, Memphis, TN 38105, USA.

出版信息

Bioorg Med Chem. 2007 Jun 1;15(11):3801-17. doi: 10.1016/j.bmc.2007.03.012. Epub 2007 Mar 12.

DOI:10.1016/j.bmc.2007.03.012
PMID:17399985
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1995442/
Abstract

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.

摘要

我们合成并评估了对称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。大多数后者是CE的优秀抑制剂，然而出乎意料的是，氟代苯偶姻是非常好的酶抑制剂。对于氟代苯偶姻的衍生K(i)值，观察到与羟基碳原子上的电荷、羰基氧以及哈米特常数呈正相关。

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Inhibition of carboxylesterases by benzil (diphenylethane-1,2-dione) and heterocyclic analogues is dependent upon the aromaticity of the ring and the flexibility of the dione moiety.联苯甲酰（二苯基乙烷-1,2-二酮）及其杂环类似物对羧酸酯酶的抑制作用取决于环的芳香性和二酮部分的柔韧性。
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Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.新型苯偶酰（二苯基乙烷-1,2-二酮）类似物作为哺乳动物羧酸酯酶抑制剂的鉴定与表征
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