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ID: ALA1137588
Journal: Bioorg Med Chem Lett
Title: An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.
Authors: Iyengar RR, Lynch JK, Mulhern MM, Judd AS, Freeman JC, Gao J, Souers AJ, Zhao G, Wodka D, Doug Falls H, Brodjian S, Dayton BD, Reilly RM, Swanson S, Su Z, Martin RL, Leitza ST, Houseman KA, Diaz G, Collins CA, Sham HL, Kym PR.
Abstract: The optimization of potent MCHr1 antagonist 1 with respect to improving its in vitro profile by replacement of the 3,4-methylenedioxy phenyl (piperonyl) moiety led to the discovery of 19, a compound that showed excellent MCHr1 binding and functional potencies in addition to possessing superior hERG separation, CYP3A4 profile, and receptor cross-reactivity profiles.
CiteXplore: 17234405