Synthesis and biological activity of a novel class nicotinic acetylcholine receptors (nAChRs) ligands structurally related to anatoxin-a |
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Authors: | Simoni Daniele Rondanin Riccardo Marchetti Paolo Rullo Cinzia Baruchello Riccardo Grisolia Giuseppina Barbato Giuseppina Giovannini Riccardo Marchioro Carla Capelli Anna Maria Virginio Caterina Bozzoli Andrea Borea Pier Andrea Merighi Stefania Donati Daniele |
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Institution: | Department of Pharmaceutical Sciences, University of Ferrara, Via Fossato di Mortara 17/19, 44121 Ferrara, Italy. smd@unife.it |
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Abstract: | The introduction of the isoxazole ring as bioisosteric replacement of the acetyl group of anatoxin-a led to a new series of derivatives binding to nicotinic acetylcholine receptors. Bulkier substitutions than methyl at the 3 position of isoxazole were shown to be detrimental for the activity. The binding potency of the most interesting compounds with α1, α7 and α3β4 receptor subtypes, was, anyway, only at micromolar level. Moreover, differently from known derivatives with pyridine, isoxazole condensed to azabicyclo ring led to no activity. |
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Keywords: | Nicotinic acetylcholine receptors ligands Anatoxin-a derivatives Therapeutic agents for CNS degenerative disorders |
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