Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils
| Autor: | Lyudmila Tsurkan, Carol C. Edwards, Monika Wierdl, Antonio M. Ferreira, Janice L. Hyatt, Latorya D. Hicks, Teri Moak, Philip M. Potter, Randy M. Wadkins |
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| Rok vydání: | 2007 |
| Předmět: |
Hydrocarbons
Fluorinated Molecular model Stereochemistry Clinical Biochemistry Quantitative Structure-Activity Relationship Pharmaceutical Science chemistry.chemical_element Phenylglyoxal Biochemistry Chemical synthesis Oxygen Article Carboxylesterase Benzoin Drug Discovery Humans Enzyme Inhibitors Molecular Biology Diketone chemistry.chemical_classification biology Chemistry Organic Chemistry In vitro Enzyme Enzyme inhibitor biology.protein Molecular Medicine Carboxylic Ester Hydrolases |
| Zdroj: | Bioorganic & Medicinal Chemistry. 15:3801-3817 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2007.03.012 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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