Discovery, synthesis and biological characterization of a series of N-(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1H-pyrazol-5-yl)acetamide ethers as novel GIRK1/2 potassium channel activators
Literature Information
Publication Date
2021-06-21
DOI
10.1039/D1MD00129A
Impact Factor
0
Authors
Swagat Sharma, Lauren Lesiak, Christopher D. Aretz, Yu Du, Sushil Kumar, Nagsen Gautam, Yazen Alnouti, Nikilesh V. Dhuria, Yashpal S. Chhonker, C. David Weaver, Corey R. Hopkins
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Abstract
The present study describes the discovery and characterization of a series of N-(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1H-pyrazol-5-yl)acetamide ethers as G protein-gated inwardly-rectifying potassium (GIRK) channel activators. From our previous lead optimization efforts, we have identified a new ether-based scaffold and paired this with a novel sulfone-based head group to identify a potent and selective GIRK1/2 activator. In addition, we evaluated the compounds in tier 1 DMPK assays and have identified compounds that display nanomolar potency as GIRK1/2 activators with improved metabolic stability over the prototypical urea-based compounds.
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