1185503-38-1Relevant articles and documents
Optimization of piperidin-4-yl-urea-containing melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Reducing hERG-associated liabilities
Berglund, Susanne,Egner, Bryan J.,Graden, Henrik,Graden, Joakim,Morgan, David G.A.,Inghardt, Tord,Giordanetto, Fabrizio
scheme or table, p. 4274 - 4279 (2010/04/26)
The discovery and optimization of piperidin-4-yl-urea derivatives as MCH-R1 antagonists is herein described. Previous work around the piperidin-4-yl-amides led to the discovery of potent MCH-R1 antagonists. However, high affinity towards the hERG potassium channel proved to be an issue. Different strategies to increase hERG selectivity were implemented and resulted in the identification of piperidin-4-yl-urea compounds as potent MCH-R1 antagonists with minimized hERG inhibition.