Discovery and development of a novel class of phenoxyacetyl amides as highly potent TRPM8 agonists for use as cooling agents
作者:Alain Noncovich、Chad Priest、Jane Ung、Andrew P. Patron、Guy Servant、Paul Brust、Nicole Servant、Nathan Faber、Hanghui Liu、Nicole S. Gonsalves、Tanya L. Ditschun
DOI:10.1016/j.bmcl.2017.04.003
日期:2017.8
The paper presents the activity trends for a novel series of phenoxyacetyl amides as human TRPM8 receptor agonists. This series encompasses in vitro activity values ranging from the micromolar to the picomolar levels. Sensory evaluation of these molecules highlights their relevance as cooling agents for oral applications. The positive outcome of the complete evaluation of N-(1H-pyrazol-3-yl)-N-(th
H5N1virus, one subtype of highly pathogenic influenza A virus in human infection, has recently received attention due to its unpredictable and high mortality. In this study, a series of arylsulfonamide derivatives were identified as improved H5N1inhibitors for the influenza treatment by systematic structure-activity relationship investigation. Among them, the most potent H5N1inhibitor 3h exhibited
Methyl-triflate-mediated dearylmethylation of <i>N</i>-(arylmethyl)carboxamides <i>via</i> the retro-Mannich reaction induced by electrophilic dearomatization/rearomatization in an aqueous medium at room temperature
Dearylmethylation of N-(arylmethyl)carboxamides was achieved under metal-free conditions in an aqueous medium induced by electrophilic dearomatization/rearomatization.
The present invention relates to compounds of structural formula I: I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.