Synthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT1A receptor
Autor
Pessoa-Mahana H.
González-Lira C.
Fierro A.
Zapata-Torres G.
Pessoa-Mahana C.D.
Ortiz-Severin J.
Iturriaga-Vásquez P.
Reyes-Parada M.
Silva-Matus P.
Saitz-Barría C.
Araya-Maturana R.
Resumen
A series of 3-(3-(4-(3-(1H-indol-3-yl)propyl)piperazin-1-yl)propyl)-1H- indole derivatives (3a-d and 5a-f) as homo- and hetero-bis-ligands, were synthesized and evaluated for in vitro affinity at the serotonin transporter (SERT) and the 5-HT1A receptor. Compounds 5b and 5f showed nanomolar affinities for both targets. The experimental data were rationalized according to results obtained from docking experiments. These findings are in agreement with our proposal that bis-indole derivatives can bind both targets, and might serve as leads in the quest of ligands endowed with a dual mechanism of action. © 2013 Elsevier Ltd. All rights reserved.
Colecciones
Ítems relacionados
Mostrando ítems relacionados por Título, autor o materia.
-
Article
Synthesis and Docking of Novel 3-Indolylpropyl Derivatives as New Polypharmacological Agents Displaying Affinity for 5-HT1AR/SERT (2020)
Pessoa-Mahana H.; Silva-Matus P.; Pessoa-Mahana C.D.; Chung H.; Iturriaga-Vásquez P.; Quiroz G.; Möller-Acuña P.; Zapata-Torres G.; Saitz-Barría C.; Araya-Maturana R.; ... (Wiley-VCH Verlag, 2017) -
Article
Synthesis, 5-hydroxytryptamine1A receptor affinity and docking studies of 3-[3-(4-aryl-1-piperazinyl)-propyl]-1H-indole derivatives (2020)
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. (Pharmaceutical Society of Japan, 2012) -
Article
Synthesis of novel nicotinic ligands with multimodal action: Targeting Acetylcholine α4β2, Dopamine and Serotonin Transporters (2020)
González-Gutiérrez J.P.; Pessoa-Mahana H.A.; Iturriaga-Vásquez P.E.; Reyes-Parada M.I.; Guerra-Díaz N.E.; Hodar-Salazar M.; Viscarra F.; Paillali P.; Núñez-Vivanco G.; Lorca-Carvajal M.A.; ... (MDPI AG, 2019)