Synthesis, 5-Hydroxytryptamine1A Receptor Affinity and Docking Studies of 3-[3-(4-Aryl-1-piperazinyl)-propyl]-1H-Indole Derivatives
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概要
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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 (IC50=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.
- 公益社団法人 日本薬学会の論文
著者
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Pessoa-Mahana Hernán
Departments of Organic and Physical Chemistry, Faculty of Chemical and Pharmaceutical Sciences, University of Chile
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Núñez Catalina
Departments of Organic and Physical Chemistry, Faculty of Chemical and Pharmaceutical Sciences, University of Chile
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Araya-Maturana Ramiro
Departments of Organic and Physical Chemistry, Faculty of Chemical and Pharmaceutical Sciences, University of Chile
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Barría Claudio
Departments of Organic and Physical Chemistry, Faculty of Chemical and Pharmaceutical Sciences, University of Chile
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Zapata-Torres Gerald
Analytical and Inorganic Chemistry, Faculty of Chemical and Pharmaceutical Sciences, University of Chile
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Pessoa-Mahana Carlos
Department of Pharmacy, Faculty of Chemistry, Pontificia Universidad Católica de Chile
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Iturriaga-Vasquez Patricio
Millennium Institute for Cell Dynamics and Biotechnology
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Mella-Raipán Jaime
Department of Pharmacy, Faculty of Chemistry, Pontificia Universidad Católica de Chile
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Reyes-Parada Miguel
Millennium Institute for Cell Dynamics and Biotechnology
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Celis-Barros Cristian
Analytical and Inorganic Chemistry, Faculty of Chemical and Pharmaceutical Sciences, University of Chile
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Mella-Raipán Jaime
Department of Pharmacy, Faculty of Chemistry, Pontificia Universidad Católica de Chile
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Pessoa-Mahana Carlos
Department of Pharmacy, Faculty of Chemistry, Pontificia Universidad Católica de Chile
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Barría Claudio
Departments of Organic and Physical Chemistry, Faculty of Chemical and Pharmaceutical Sciences, University of Chile