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Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity |
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| Authors: | Judd Andrew S Souers Andrew J Wodka Dariusz Zhao Gang Mulhern Mathew M Iyengar Rajesh R Gao Ju Lynch John K Freeman Jennifer C Falls H Douglas Brodjian Sevan Dayton Brian D Reilly Regina M Gintant Gary Limberis James T Mikhail Ann Leitza Sandra T Houseman Kathryn A Diaz Gilbert Bush Eugene N Shapiro Robin Knourek-Segel Victoria Hernandez Lisa E Marsh Kennan C Sham Hing L Collins Christine A Kym Philip R |
| Affiliation: | Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. andrew.judd@abbott.com |
| 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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