4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists

…, P Lin, M Hoang, L Chang, C Tan, S Feighner…

Index: Jiang, Jinlong; Lin, Peter; Hoang, Myle; Chang, Lehua; Tan, Carina; Feighner, Scott; Palyha, Oksana C.; Hreniuk, Donna L.; Pan, Jie; Sailer, Andreas W.; Morin, Nancy R.; MacNeil, Douglas J.; Howard, Andrew D.; Van der Ploeg, Lex H.T.; Goulet, Mark T.; DeVita, Robert J. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 20 p. 5275 - 5279

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Citation Number: 9

Abstract

Structure–activity relationships of a 4-aminoquinoline MCH1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6- position. Modifications of the 4-amino group were not well tolerated.