62649-36-9Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Page/Page column 19, (2012/11/08)
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
Pyrazolo-[1,5-a]-Pyrimidones Derivatives and Pharmaceutical Compositions and Uses Thereof
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Page/Page column 7, (2012/04/18)
The present invention provides new pyrazolo-[1,5-a]-pyrimidone derivates and pharmaceutical compositions comprising said compounds and one or more pharmaceutically acceptable carriers or diluents. The uses of the compounds for the manufacture of potassium
Design, synthesis and biological activity of pyrazolo[1,5-a]pyrimidin-7(4H) -ones as novel Kv7/KCNQ potassium channel activators
Qi, Jinlong,Zhang, Fan,Mi, Yi,Fu, Yan,Xu, Wen,Zhang, Diqun,Wu, Yibing,Du, Xiaona,Jia, Qingzhong,Wang, Kewei,Zhang, Hailin
experimental part, p. 934 - 943 (2011/04/17)
Voltage-gated Kv7/KCNQ/M-potassium channels play a pivotal role in controlling neuronal excitability. Genetic reduction of KCNQ channel activity as a result of mutations causes various human diseases such as epilepsy and arrhythmia. Therefore, discovery of small molecules that activate KCNQ channels is an important strategy for clinical intervention of membrane excitability related disorders. In this study, a series of pyrazolo[1,5-a]pyrimidin-7(4H)- ones (PPOs) have been found to be novel activators (openers) of KCNQ2/3 potassium channels through high-throughput screening by using atomic absorption rubidium efflux assay. Based on structure-activity relationship (SAR), the substituted PPOs have been optimized. The 5-(2,6-dichloro-5-fluoropyridin-3-yl)- 3-phenyl-2-(trifluoromethyl) pyrazolo[1,5-a]pyrimidin-7(4H)-one (17) was identified as a novel, potent, and selective KCNQ2/3 potassium channel opener by patch-clamp recording assay.
