Synthesis and receptor binding studies of some new arylcarboxamide derivatives as sigma-1 ligands期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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Synthesis and receptor binding studies of some new arylcarboxamide derivatives as sigma-1 ligands

Institution:	1. Department of Chemistry & Pharmaceutical Sciences, Piazzale Europa 1, University of Trieste, 34127 Trieste, Italy;2. Molecular Simulation Engineering (MOSE) Laboratory, DI3, Piazzale Europa 1, University of Trieste, 34127 Trieste, Italy;1. Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi ‘Aldo Moro’ di Bari, Via Orabona 4, 70126 Bari, Italy;2. Università degli Studi di Firenze, Dipartimento di Chimica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy;3. Università degli Studi di Firenze, Neurofarba Dept., Section of Pharmaceutical and Nutriceutical Sciences, Via U. Schiff 6, 50019 Sesto Fiorentino (Firenze), Italy;1. CNRS, SRSMC, UMR 7565, Vandœuvre-lès-Nancy, F-54506, France;2. Université de Lorraine, SRSMC, UMR 7565, Nancy F-54001, France;3. ABC Platform®, Nancy F-54001, France;1. Department of Chemistry, Indian Institute of Technology Bombay, Mumbai 400076, India;2. Discipline of Chemistry, Indian Institute of Technology Indore, Indore 452 017, India;1. Faculty of Agriculture, Ehime University, 3-5-7 Tarumi, Matsuyama, Ehime 790-8566, Japan;2. South Ehime Fisheries Research Center, 1289-1 Funakoshi, Ainan, Ehime 798-4292, Japan;3. Integrated Center for Sciences, Tarumi Station, Ehime University, 3-5-7 Tarumi, Matsuyama, Ehime 790-8566, Japan;1. Department of Gastroenterology, Kochi Medical School, Kochi, Japan;2. Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy;3. Department of Chemistry, College of Science, King Saud University, PO Box 2455, Riyadh 11451, Saudi Arabia;4. Istituto di Biochimica delle Proteine—CNR, Via P. Castellino 111, 80131 Napoli, Italy;5. Università degli Studi di Firenze, Polo Scientifico, Dipartimento di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy

Abstract:	We describe here the synthesis and the binding interaction with σ₁ and σ₂ receptors of a series of new arylcarboxamide derivatives variously substituted on the aromatic portions. Maintaining a partial scaffold of a series of compounds previously synthesized by us, we evaluate the effect of the substitution on σ binding. The synthesized compounds have been tested to estimate their affinity and selectivity toward σ₁ and σ₂ receptors. Two out of 16 derivatives showed an interesting σ₁ affinity (21.2 and 13.6 nM—compounds 2m and 2p) and a good selectivity (K_i(σ₂)/K_i(σ₁) >140 and >40, respectively).

Keywords:	σ-Receptors Arylcarboxamide derivatives Radioligand binding assays
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