Referenced in: none

Automatically associated channels: Kv11.1

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

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

Journal, date & volume: Bioorg. Med. Chem. Lett., 2007 Feb 15 , 17, 874-8

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/17234405

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.