An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists |
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| Authors: | Iyengar Rajesh R Lynch John K Mulhern Mathew M Judd Andrew S Freeman Jennifer C Gao Ju Souers Andrew J Zhao Gang Wodka Dariusz Doug Falls H Brodjian Sevan Dayton Brian D Reilly Regina M Swanson Sue Su Zhi Martin Ruth L Leitza Sandra T Houseman Kathryn A Diaz Gilbert Collins Christine A Sham Hing L Kym Philip R |
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| Institution: | Metabolic Disease Research, Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. rajesh.iyengar@abbott.com |
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| 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. |
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