113984-70-6Relevant articles and documents
New insight into the application of GFP chromophore inspired derivatives: A F- fluorescent chemodosimeter
Liu, Xiao-Yuan,Shi, Lei,Ding, Zhifeng,Long, Yi-Tao
, p. 53557 - 53560 (2014)
A GFP chromophore inspired fluorescent chemodosimeter was synthesized, which exhibited naked-eye detection for F- with high selectivity and sensitivity based on F- promoted cleavage of silicon-oxygen bonds and the deprotonation reaction via hydrogen-bonding interactions. This journal is
Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists
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.
, p. 4957 - 4977 (2020/05/25)
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.
2,5-Dihydroxybenzyl and (1,4-dihydroxy-2-naphthyl)methyl, novel reductively armed photocages for the hydroxyl moiety
Kostikov, Alexey P.,Popik, Vladimir V.
, p. 9190 - 9194 (2008/03/14)
(Chemical Equation Presented) Irradiation of alcohols, phenols, and carboxylic acids "caged" with the 2,5-dihydroxybenzyl group or its naphthalene analogue results in the efficient release of the substrate. The initial byproduct of the photoreaction, 4-hydroxyquinone-2-methide, undergoes rapid tautomerization into methyl p-quinone. The UV spectrum of the latter is different from that of the caging chromophore, thus permitting selective irradiation of the starting material in the presence of photochemical products. These photoremovable protecting groups can be armed in situ by the reduction of photochemically inert p-quinone precursors.