Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1366851 | Bioorganic & Medicinal Chemistry Letters | 2007 | 7 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
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,