IMPAM 23988
INSTITUTO DE INVESTIGACIONES EN MICROBIOLOGIA Y PARASITOLOGIA MEDICA
Unidad Ejecutora - UE
artículos
Título:
Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase
Autor/es:
G. C. MUSCIA; S. HAUTMANN; G. BULDAIN; S. ASIS; M. GUTSCHOW
Revista:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Editorial:
PERGAMON-ELSEVIER SCIENCE LTD
Referencias:
Lugar: Amsterdam; Año: 2014 vol. 24 p. 1545 - 1549
ISSN:
0960-894X
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 ìM) was characterized as a mixed-type inhibitor with a pronounced competitive binding mode
