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

Authors :
Dodd CJ
Chronister KS
Rathnayake U
Parr LC
Li K
Chang S
Mi D
Days EL
Bauer JA
Cho HP
Boutaud O
Denton JS
Lindsley CW
Han C
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2023 May 01; Vol. 87, pp. 129256. Date of Electronic Publication: 2023 Mar 24.
Publication Year :
2023

Abstract

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.<br />Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2023 Elsevier Ltd. All rights reserved.)

Subjects

Subjects :
Sulfonylurea Receptors metabolism

Details

Language :
English
ISSN :
1464-3405
Volume :
87
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
36966977
Full Text :
https://doi.org/10.1016/j.bmcl.2023.129256