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

Bioorganic & medicinal chemistry letters 2023 May 01

filter terms:

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. Copyright © 2023 Elsevier Ltd. All rights reserved.

Citation

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. Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS. Bioorganic & medicinal chemistry letters. 2023 May 01;87:129256