Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS

Cayden J. Dodd,Keagan S. Chronister,Upendra Rathnayake,Lauren C. Parr,Kangjun Li,Sichen Chang,Dehui Mi,Emily L. Days,Joshua A. Bauer,Hyekyung P. Cho,Olivier Boutaud,Jerod S. Denton,Craig W. Lindsley,Changho Han

Bioorganic & Medicinal Chemistry Letters（2023）

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摘要

Kir6.2/SUR1 is an ATP-regulated potassium channel that acts as an intracellular metabolic sensor, controlling insulin and appetite-stimulatory neuropeptides secretion. In this Letter, we present the SAR around a novel Kir6.2/SUR1 channel opener scaffold derived from an HTS screening campaign. New series of compounds with tractable SAR trends and favorable potencies are reported.

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关键词

Channel opener,Insulin homeostasis,K(ATP) Channels,Kir6.2/SUR1,Structure-Activity Relationship (SAR)

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