Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands

…, SW Topiol, SB Poda, Y Ren, G Chandrasena…

Index: Li, Guiying; Zhou, Hao; Jiang, Yu; Keim, Holger; Topiol, Sidney W.; Poda, Suresh B.; Ren, Yong; Chandrasena, Gamini; Doller, Dario Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 4 p. 1236 - 1242

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Citation Number: 11

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.