Bioorganic and Medicinal Chemistry Letters p. 791 - 796 (2019)
Update date:2022-08-04
Topics:
Sharma, Swagat
Kozek, Krystian A.
Abney, Kristopher K.
Kumar, Sushil
Gautam, Nagsen
Alnouti, Yazen
David Weaver
Hopkins, Corey R.
The present study describes the discovery and characterization of a series of 5-aryl-2H-tetrazol-3-ylacetamides as G protein-gated inwardly-rectifying potassium (GIRK) channels activators. Working from an initial hit discovered during a high-throughput screening campaign, we identified a tetrazole scaffold that shifts away from the previously reported urea-based scaffolds while remaining effective GIRK1/2 channel activators. In addition, we evaluated the compounds in Tier 1 DMPK assays and have identified a (3-methyl-1H-pyrazol-1-yl)tetrahydrothiophene-1,1-dioxide head group that imparts interesting and unexpected microsomal stability compared to previously-reported pyrazole head groups.
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