716361-59-0Relevant academic research and scientific papers
ACTIVATOR OF TREK (TWIK RELATED K+ CHANNELS) CHANNELS
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Paragraph 0298; 0300, (2018/07/05)
Disclosed is a compound of formula (I): wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the c
Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: Effect of sulfonamides P3 substituents on potency and selectivity
Ayesa, Susana,Lindquist, Charlotta,Agback, Tatiana,Benkestock, Kurt,Classon, Bjoern,Henderson, Ian,Hewitt, Ellen,Jansson, Katarina,Kallin, Anders,Sheppard, Dave,Samuelsson, Bertil
experimental part, p. 1307 - 1324 (2009/08/08)
Highly potent and selective 4-amidofuran-3-one inhibitors of cathepsin S are described. The synthesis and structure-activity relationship of a series of inhibitors with a sulfonamide moiety in the P3 position is presented. Several members of the series show sub-nanomolar inhibition of the target enzyme as well as an excellent selectivity profile and good cellular potency. Molecular modeling of the most interesting inhibitors describes interactions in the extended S3 pocket and explains the observed selectivity towards cathepsin K.
