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

✍ Scribed by Guiying Li; Hao Zhou; Yu Jiang; Holger Keim; Sidney W. Topiol; Suresh B. Poda; Yong Ren; Gamini Chandrasena; Darío Doller


Book ID
104005244
Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
561 KB
Volume
21
Category
Article
ISSN
0960-894X

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✦ Synopsis


Two series of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives exhibiting diverse functionality at rat MT(1) and MT(2) receptors are reported. Compounds 11f and 18b (MT(1)/MT(2) agonist) have human microsomal intrinsic clearance comparable to ramelteon.


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