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Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands
Authors:Li Guiying  Zhou Hao  Jiang Yu  Keim Holger  Topiol Sidney W  Poda Suresh B  Ren Yong  Chandrasena Gamini  Doller Darío
Institution:a Department of Chemical & Pharmacokinetic Sciences, Lundbeck Research USA, 215 College Rd., Paramus, NJ 07652, USA
b Department of Biological Research, Lundbeck Research USA, 215 College Rd., Paramus, NJ 07652, USA
Abstract:Two series of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives exhibiting diverse functionality at rat MT1 and MT2 receptors are reported. Compounds 11f and 18b (MT1/MT2 agonist) have human microsomal intrinsic clearance comparable to ramelteon.
Keywords:WHNBFHNVGXNLCB-UHFFFAOYSA-N  IQYNIMPSBOGDGR-ZDUSSCGKSA-N
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