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dc.contributor.author
Muscia, Gisela Celeste
dc.contributor.author
Hautmann, Stephanie
dc.contributor.author
Buldain, Graciela Yolanda
dc.contributor.author
Asís, Silvia Elizabeth
dc.contributor.author
Gütschow, Michael
dc.date.available
2017-05-15T22:12:42Z
dc.date.issued
2014-03
dc.identifier.citation
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
dc.identifier.issn
0960-894X
dc.identifier.uri
http://hdl.handle.net/11336/16525
dc.description.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.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Elsevier
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.subject
Cholesterol Esterase
dc.subject
Quinolines
dc.subject
Friedländer Reaction
dc.subject
Mixed-Type Inhibition
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Química Orgánica
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2017-05-15T14:44:17Z
dc.journal.volume
24
dc.journal.number
6
dc.journal.pagination
1545-1549
dc.journal.pais
Países Bajos
dc.journal.ciudad
Ámsterdam
dc.description.fil
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
dc.description.fil
Fil: Hautmann, Stephanie. Universitaet Bonn; Alemania
dc.description.fil
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
dc.description.fil
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
dc.description.fil
Fil: Gütschow, Michael. Universitaet Bonn; Alemania
dc.journal.title
Bioorganic & Medicinal Chemistry Letters
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0960894X14001218
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.bmcl.2014.01.081
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