100727-17-1Relevant articles and documents
Human iPSC-derived cardiomyocytes and pyridyl-phenyl mexiletine analogs
Cashman, John R.,Gomez-Galeno, Jorge,Johnson, Mark,Kass, Robert S.,McKeithan, Wesley L.,Mercola, Mark,Okolotowicz, Karl,Ryan, Daniel,Sampson, Kevin J.
supporting information, (2021/06/15)
In the United States, approximately one million individuals are hospitalized every year for arrhythmias, making arrhythmias one of the top causes of healthcare expenditures. Mexiletine is currently used as an antiarrhythmic drug but has limitations. The purpose of this work was to use normal and Long QT syndrome Type 3 (LQTS3) patient-derived human induced pluripotent stem cell (iPSC)-derived cardiomyocytes to identify an analog of mexiletine with superior drug-like properties. Compared to racemic mexiletine, medicinal chemistry optimization of substituted racemic pyridyl phenyl mexiletine analogs resulted in a more potent sodium channel inhibitor with greater selectivity for the sodium over the potassium channel and for late over peak sodium current.
HALOGENATION AND NITRATION OF 2-PYRIDONES
Faidallah, Hassan M.
, p. 281 - 288 (2007/10/02)
Halogenation of the 2-pyridones 2 afforded the corresponding mono-di- or tri-halo derivative depending on the conditions of the reaction.Nitration of 2a gave the dinitro-2-pyridone 4k, while nitration of 2c yielded the 3-nitro derivative 4p.Structures were confirmed by spectral data.
