Referenced in: none

Automatically associated channels: Kv11.1

Title: Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.

Authors: Andrew S Judd, Andrew J Souers, Dariusz Wodka, Gang Zhao, Mathew M Mulhern, Rajesh R Iyengar, Ju Gao, John K Lynch, Jennifer C Freeman, H Douglas Falls, Sevan Brodjian, Brian D Dayton, Regina M Reilly, Gary Gintant, James T Limberis, Ann Mikhail, Sandra T Leitza, Kathryn A Houseman, Gilbert Diaz, Eugene N Bush, Robin Shapiro, Victoria Knourek-Segel, Lisa E Hernandez, Kennan C Marsh, Hing L Sham, Christine A Collins, Philip R Kym

Journal, date & volume: Bioorg. Med. Chem. Lett., 2007 Apr 15 , 17, 2365-71

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/17350253

Abstract
A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human Ether-a-go-go Related Gene) channel affinity and functional blockade. Basic dialkylamine-terminated analogs were found to weakly bind the hERG channel and provided marked improvement in a functional patch-clamp assay versus previously reported antagonists of the series.