Artículos de revistas
Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase
Fecha
2014-03Registro en:
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
0960-894X
Autor
Muscia, Gisela Celeste
Hautmann, Stephanie
Buldain, Graciela Yolanda
Asís, Silvia Elizabeth
Gütschow, Michael
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.