Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase
| Autor: | Gisela Celeste Muscia, Silvia E. Asis, Stephanie Hautmann, Michael Gütschow, Graciela Buldain |
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| Rok vydání: | 2014 |
| Předmět: |
Swine
Stereochemistry Clinical Biochemistry Pharmaceutical Science Binding Competitive Biochemistry Structure-Activity Relationship chemistry.chemical_compound Cysteine Proteases Competitive binding Drug Discovery Mixed-type inhibition Animals Humans Friedländer reaction Enzyme Inhibitors Microwaves Molecular Biology Cholesterol Esterase Chemistry Organic Chemistry Quinoline Ciencias Químicas Sterol Esterase Cholesterol esterase Enzyme Activation Kinetics Química Orgánica Quinolines Molecular Medicine Cattle CIENCIAS NATURALES Y EXACTAS Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 24:1545-1549 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2014.01.081 |
| Popis: | 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. Fil: Muscia, Gisela Celeste. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Química Orgánica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Hautmann, Stephanie. Universitaet Bonn; Alemania Fil: Buldain, Graciela Yolanda. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Química Orgánica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Asís, Silvia Elizabeth. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Química Orgánica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Gütschow, Michael. Universitaet Bonn; Alemania |
| Databáze: | OpenAIRE |
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