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Synthesis and Biological Screening of Novel Indolalkyl Arenes Targeting the Serotonine Transporter

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 (Ki = 33.0, 48.0, and 17 nM, respectively). The other synthesized compounds showed moderate or no affinity in the binding studies.

The affinities for the serotonin transporter of a new series of functionalized indolylalkylarenes 3–16(a and b) were investigated in vitro. With Ki values of 33.0, 48.0, and 17 nM, compounds 3b, 4b, and 5b, respectively, showed good binding affinities. The other synthesized compounds showed moderate or no affinity in the binding studies.

Autoren:   Claudia Ojeda‐Gómez, Hernán Pessoa‐Mahana, Patricio Iturriaga‐Vásquez, Carlos David Pessoa‐Mahana, Gonzalo Recabarren‐Gajardo, Claudio Méndez‐Rojas
Journal:   Archiv der Pharmazie
Jahrgang:   2013
Seiten:   n/a
DOI:   10.1002/ardp.201300321
Erscheinungsdatum:   11.12.2013
Fakten, Hintergründe, Dossiers
  • Serotonin
  • Substitution
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