Optimization of piperidin-4-yl-urea-containing melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Reducing hERG-associated liabilities

DOI: 10.1016/j.bmcl.2009.05.066

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 4274 - 4279 (2009)

Update date:2022-08-03

Topics:

Authors:

Berglund, Susanne

Egner, Bryan J.

Graden, Henrik

Graden, Joakim

Morgan, David G.A.

Inghardt, Tord

Giordanetto, Fabrizio

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Article abstract of DOI:10.1016/j.bmcl.2009.05.066

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.

Full text of DOI:10.1016/j.bmcl.2009.05.066

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