Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase |
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| Affiliation: | 1. Departamento de Química Orgánica, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín 956, Ciudad Autónoma de Buenos Aires C1113AAB, Argentina;2. Pharmaceutical Institute, University of Bonn, An der Immenburg 4, Bonn D-53115, Germany;1. School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, POB 1627, 70211 Kuopio, Finland;2. Departments of Pharmacology and Toxicology and Psychiatry, University of Toronto, Campbell Family Mental Health Research Institute, M5S 1A8 Toronto, Ontario, Canada |
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| Abstract: | A series of 2-(substituted) phenyl and 2-indolyl quinoline derivatives (10a–l) was synthesized by an efficient microwave-assisted, trifluoroacetic acid-catalyzed, solvent-free method. Evaluation of the inhibitory activity led to the identification of two quinoline inhibitors of cholesterol esterase. 2-(1H-Indol-3-yl)-6-nitro-4-phenylquinoline (10l; IC50 = 1.98 μM) was characterized as a mixed-type inhibitor with a pronounced competitive binding mode. |
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| Keywords: | Friedländer reaction Cholesterol esterase Quinolines Mixed-type inhibition |
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