52109-85-0Relevant articles and documents
Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold
Flaherty, Daniel P.,Simpson, Denise S.,Miller, Melissa,Maki, Brooks E.,Zou, Beiyan,Shi, Jie,Wu, Meng,McManus, Owen B.,Aubé, Jeffrey,Li, Min,Golden, Jennifer E.
, p. 3968 - 3973 (2014/09/03)
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 physiological 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 IC 50 = 16 nM with 62-fold selectivity over TASK-3 in an orthogonal electrophysiology assay.
Facile and effective synthesis of N-aryl-2-furancarboxamides derivatives under the condition of phase transfer catalysis
Wei, Tai-Bao,Zhang, You-Ming
, p. 2943 - 2947 (2007/10/03)
A convenient one-pot procedure is reported for the preparation of N- aryl-2-furancarboxamide derivatives. 2-Furoic acid is activated by benzenesulfonyl chloride under the condition of solid-liquid phase transfer catalysis using solid potassium carbonate a
