Synthesis of new N-(arylcyclopropyl) acetamides and N-(arylvinyl) acetamides as conformationally-restricted ligands for melatonin receptors

…, P Renard, P Delagrange, M Mathé-Allainmat

Index: Morellato, Laurence; Lefas-Le Gall, Marie; Langlois, Michel; Caignard, Daniel-Henri; Renard, Pierre; Delagrange, Philippe; Mathe-Allainmat, Monique Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 2 p. 430 - 434

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Citation Number: 8

Abstract

N-(Arylcyclopropyl) acetamides and N-(arylvinyl) acetamides or methyl ureas have been prepared as constrained analogues of melatonin. The affinity of these new compounds for chicken brain melatonin receptors and recombinant human MT1 and MT2 receptors was evaluated using 2-[125I]-iodomelatonin as radioligand. Strict ethylenic or cyclopropyl analogues of the commercialized agonist agomelatine (Valdoxan®) were equipotent to ...

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