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ID: ALA1137266
Journal: Bioorg Med Chem Lett
Title: 4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists.
Authors: Jiang J, Lin P, Hoang M, Chang L, Tan C, Feighner S, Palyha OC, Hreniuk DL, Pan J, Sailer AW, Morin NR, MacNeil DJ, Howard AD, Van der Ploeg LH, Goulet MT, DeVita RJ.
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.
CiteXplore: 16919453