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Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists

Author:
Fotsing, Joseph R.  Darmohusodo, Vincent  Patron, Andrew P.  Ching, Brett W.  Brady, Thomas  Arellano, Melissa  Chen, Qing  Davis, Timothy J.  Liu, Hanghui  Servant, Guy  Zhang, Lan  Williams, Mark  Saganich, Michael  Ditschun, Tanya  Tachdjian, Catherine  Karanewsky, Donald S.  


Journal:
JOURNAL OF MEDICINAL CHEMISTRY


Issue Date:
2020


Abstract(summary):

In humans, bitter taste is mediated by 25 TAS2Rs. Many compounds, including certain active pharmaceutical ingredients, excipients, and nutraceuticals, impart their bitter taste (or in part) through TAS2R8 activation. However, effective TAS2R8 blockers that can either suppress or reduce the bitterness of these compounds have not been described. We are hereby reporting a series of novel 3-(pyrazol-4-yl) imidazolidine-2,4-diones as potent and selective TAS2R8 antagonists. In human sensory tests, S6821 and S7958, two of the most potent analogues from the series, demonstrated efficacy in blocking TAS2R8-mediated bitterness and were selected for development. Following data evaluation by expert panels of a number of national and multinational regulatory bodies, including the US, the EU, and Japan, S6821 and S7958 were approved as safe under conditions of intended use as bitter taste blockers.


Page:
4957---4977


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