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

作者：Hicks Latorya D; Hyatt Janice L; Moak Teri; Edwards Carol C; Tsurkan Lyudmila; Wierdl Monika; Ferreira Antonio M; Wadkins Randy M; Potter Philip M^*

来源：Bioorganic & Medicinal Chemistry, 2007, 15(11): 3801-3817.

DOI：10.1016/j.bmc.2007.03.012

• fluorobenzil
• fluorobenzoin
• carboxylesterase
• inhibitor

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.

• 出版日期2007-6-1
• 单位上海生物信息技术研究中心