Flaherty, Daniel P.; Simpson, Denise S.; Miller, Melissa; Maki, Brooks E.; Zou, Beiyan; Shi, Jie; Wu, Meng; McManus, Owen B.; Aube, Jeffrey; Li, Min; Golden, Jennifer E. published the artcile< Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold>, Recommanded Product: 2-(Trifluoromethoxy)benzoyl chloride, the main research area is bis amide derivative preparation TASK1 potassium channel inhibitor; Bis-amide; KCNK3; Selective potassium channel inhibitor; TASK1.
TASK-1 is a two-pore domain potassium channel that is important to modulating cell excitability, most notably in the context of neuronal pathways. In order to leverage TASK-1 for therapeutic benefit, its physiol. role needs better characterization; however, designing selective inhibitors that avoid the closely related TASK-3 channel has been challenging. In this study, a series of bis-amide derived compounds were found to demonstrate improved TASK-1 selectivity over TASK-3 compared to reported inhibitors. Optimization of a marginally selective hit led to analog 35 which displays a TASK-1 IC50 = 16 nM with 62-fold selectivity over TASK-3 in an orthogonal electrophysiol. assay.
Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Recommanded Product: 2-(Trifluoromethoxy)benzoyl chloride.
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics