Efficient synthesis of novel glutamate homologues and investigation of their affinity and selectivity profile at ionotropic glutamate receptors |
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| Institution: | 1. Dipartimento di Scienze Farmaceutiche DISFARM, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy;2. Dipartimento di Scienze per gli Alimenti, la Nutrizione e l’Ambiente (DeFENS), Università degli Studi di Milano, via Mangiagalli 25, 20133 Milano, Italy;3. Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen OE, Denmark;1. Department of Drug Sciences, University of Catania, V. le A. Doria 6, 95125 Catania, Italy;2. Department of Pharmacy, University of Parma, Parco Area Delle Scienze 27/A, 43124 Parma, Italy;3. Department of Physiological Sciences, University of Catania, V. le A. Doria 6, 95125 Catania, Italy;4. Department of Surgery, University of Catania, V. le A. Doria 6, 95125 Catania, Italy;1. Research Institute of Physical and Organic Chemistry, Southern Federal University, Rostov-on-Don 344090, Russia;2. Institute of General and Inorganic Chemistry, Russian Academy of Sciences, Moscow 119991, Russia;3. Southern Scientific Center, Russian Academy of Sciences, Rostov-on-Don 344006, Russia;4. Southern Federal University, Faculty of Chemistry, Rostov-on-Don 344090, Russia;1. School of Logistics Engineering, Wuhan University of Technology, China;2. School of Mechanical and Electrical Engineering, Wuhan University of Technology, China;3. School of Electronic and Information Engineering, Southwest University, China;1. CIDE, Carretera México-Toluca 3655, Col. Lomas de Santa Fe, 01210 México, D.F., Mexico;2. CIDE, Department of Economics, Carretera México-Toluca 3655, Col. Lomas de Santa Fe, 01210 México, D.F., Mexico;3. DIW Berlin, Department of Energy, Transportation, Environment, Mohrenstraße 58, 10117 Berlin, Germany;1. Department of Medicinal Chemistry and Chemical Biology, Utrecht Institute for Pharmaceutical Sciences, Faculty of Science, Utrecht University, PO Box 80082, 3508 TB Utrecht, The Netherlands;2. School of Chemistry, Joseph Black Building, University of Glasgow, University Avenue, Glasgow G12 8QQ, UK;1. Department of Chemistry, Tsinghua University, Beijing 100084, China;2. Institute of Chemical Materials, CAEP, Mianyang 621900, China |
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| Abstract: | A convenient synthesis of four new enantiomerically pure acidic amino acids is reported and their affinity at ionotropic glutamate receptors was determined. The new compounds are higher homologues of glutamic acid in which the molecular complexity has been increased by introducing an aromatic/heteroaromatic ring, that is a phenyl or a thiophene ring, that could give additional electronic interactions with the receptors. The results of the present investigation indicate that the insertion of an aromatic/heteroaromatic ring into the amino acid skeleton of glutamate higher homologues is well tolerated and this modification could be exploited to generate a new class of NMDA antagonists. |
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| Keywords: | Semi-preparative chiral HPLC Heck reaction |
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