Synthesis, 5-hydroxytryptamine1A receptor affinity and docking studies of 3-[3-(4-aryl-1-piperazinyl)-propyl]-1H-indole derivatives
Autor
Pessoa-Mahana H.
Núñez C.U.
Araya-Maturana R.
Barría C.S.
Zapata-Torres G.
Pessoa-Mahana C.D.
Iturriaga-Vasquez P.
Mella-Raipán J.
Reyes-Parada M.
Celis-Barros C.
Resumen
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.
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