Options
Synthesis, 5-Hydroxytryptamine(1a) Receptor Affinity and Docking Studies of 3-[3-(4-Aryl-1-Piperazinyl)-Propyl]-1h-Indole Derivatives
ISSN
0009-2363
Date Issued
2012
Author(s)
Araya-Maturana, Ramiro
Celis-Barros, Cristian
David Pessoa-Mahana, Carlos
Iturriaga-Vasquez, Patricio
Mella-Raipan, Jaime
Pessoa-Mahana, Hernan
Saitz Barria, Claudio
Ugarte Nunez, Catalina
Zapata-Torres, Gerald
Abstract
A series of 3-[3-(4-aryl-1-piperazinyl)-propyl]-1H-indole derivatives (12a-h) was synthesized and evaluated for binding affinity at the human 5-hydroxytryptamine1A receptor (5-HT1AR) compounds (12b) and (12h) showed the highest 5-HT1A receptor affinity (IC 50-=15 nM). Molecular docking studies with all the compounds in a homology model of 5-HT1A showed that the main interaction anchoring the ligand in the receptor was a charge-reinforced bond between the protonated nitrogen atom (N-4) of the piperazine ring and Aspartate3.32. © 2012 The Pharmaceutical Society of Japan.