Synthesis and Biological Screening of Novel Indolalkyl Arenes Targeting the Serotonine Transporter
Author
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Ojeda Gómez, Claudia
Author
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Pessoa Mahana, Hernán
es_CL
Author
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Iturriaga-Vásquez, Patricio
es_CL
Author
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Pessoa Mahana, Carlos David
es_CL
Author
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Recabarren Gajardo, Gonzalo Iván
es_CL
Author
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Méndez Rojas, Claudio
es_CL
Admission date
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2015-01-05T19:36:03Z
Available date
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2015-01-05T19:36:03Z
Publication date
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2014
Cita de ítem
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Arch. Pharm. Chem. Life Sci. 2014, 347, 174–184
en_US
Identifier
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DOI 10.1002/ardp.201300321
Identifier
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https://repositorio.uchile.cl/handle/2250/121958
General note
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Artículo de publicación ISI
en_US
Abstract
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A series of functionalized indolylalkylarenes 3–16(a and b) were synthesized and their affinities for
the serotonin transporter were investigated in vitro. Compounds 3–12(a and b) were obtained by
nucleophilic substitution of 3-(1H-indol-3-yl)propyl-4-methylbenzenesulfonates 2(a and b) with a series
of azaheterocycles. Compounds 14–16(a and b) were prepared in a two-step sequence by reaction of
3-(1H-indol-3-yl)-2-methylpropanal with substituted 1,2-phenylenediamines. Compounds 3b, 4b, and 5b
showed good binding affinities (Ki¼33.0, 48.0, and 17 nM, respectively). The other synthesized
compounds showed moderate or no affinity in the binding studies.
en_US
Patrocinador
dc.description.sponsorship
Financial support of FONDECYT under
research projects 3110082, 1090169, and 1130347.