An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists

Rajesh Iyengar ,Ju Gao,Brian D Dayton,Christine A Collins,John K Lynch,Zhi Su,Gang Zhao,Gilbert Diaz,Andrew S Judd,Sevan Brodjian,Ruth L Martin,Hing L Sham,Sue Swanson,Andrew J Souers,Jennifer C Freeman,Philip R Kym,Mathew M Mulhern,Regina M Reilly,Dariusz Wódka ,Kathryn Houseman ,Hugh D Falls ,Sandra Leitza

doi:10.1016/j.bmcl.2006.11.065

An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists

Rajesh Iyengar , Ju Gao + Show 20 more

https://doi.org/10.1016/j.bmcl.2006.11.065

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Journal: Bioorganic & Medicinal Chemistry Letters	Publication Date: Dec 1, 2006
Citations: 20

Affiliation: Metabolic Disease Research, Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA, Integrative Pharmacology, Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA

#MCHr1 Antagonist #Functional Potencies + Show 8 more

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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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