Design, synthesis, and pharmacological effects of structurally simple ligands for MT₁ and MT₂ melatonin receptors

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• 作者：Alessia Carocci ; Alessia Catalano ; Angelo Lovece ; Giovanni Lentini ; Andrea Duranti ; Valeria Lucini ; Marilou Pannacci ; Francesco Scaglione ; Carlo Franchini
• 关键词：Melatonin ; MT₁ and MT₂ receptors ; Bioisosteres ; Phenoxyalkyl amides
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：1 September 2010
• 年：2010
• 卷：18
• 期：17
• 页码：6496-6511
• 全文大小：470 K

文摘

A series of phenoxyalkyl and phenylthioalkyl amides were prepared as melatoninergic ligands. Modulation of affinity of the newly synthesized compound by applying SARs around the terminal amide moiety, the alkyl chain, and the methoxy group on the aromatic ring provides compounds with nanomolar affinity for both melatonin receptor subtypes. Affinity towards MT₁ and MT₂ receptors were modulated also exploiting chirality. The investigation of intrinsic activity revealed that all the tested compounds behave as full or partial agonists.