Artículo

Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase

Muscia, Gisela CelesteIcon ; Hautmann, Stephanie; Buldain, Graciela YolandaIcon ; Asís, Silvia Elizabeth; Gütschow, Michael
Fecha de publicación: 03/2014
Editorial: Elsevier
Revista: Bioorganic & Medicinal Chemistry Letters
ISSN: 0960-894X
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:

Resumen

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.
Palabras clave: Cholesterol Esterase , Quinolines , Friedländer Reaction , Mixed-Type Inhibition
 
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Atribución-NoComercial-SinDerivadas 2.5 Argentina (CC BY-NC-ND 2.5 AR)
Identificadores
URI: http://hdl.handle.net/11336/16525
URL: http://www.sciencedirect.com/science/article/pii/S0960894X14001218
DOI: http://dx.doi.org/10.1016/j.bmcl.2014.01.081
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Articulos(OCA HOUSSAY)
Articulos de OFICINA DE COORDINACION ADMINISTRATIVA HOUSSAY
Citación
Muscia, Gisela Celeste; Hautmann, Stephanie; Buldain, Graciela Yolanda; Asís, Silvia Elizabeth; Gütschow, Michael; Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase; Elsevier; Bioorganic & Medicinal Chemistry Letters; 24; 6; 3-2014; 1545-1549
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