- Bifunctional Molecular Photoswitches Based on Overcrowded Alkenes for Dynamic Control of Catalytic Activity in Michael Addition Reactions
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The emerging field of artificial photoswitchable catalysis has recently shown striking examples of functional light-responsive systems allowing for dynamic control of activity and selectivity in organocatalysis and metal-catalysed transformations. While o
- Pizzolato, Stefano F.,Collins, Beatrice S. L.,van Leeuwen, Thomas,Feringa, Ben L.
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supporting information
p. 6174 - 6184
(2017/05/05)
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- Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimers Disease: Design, synthesis, and characterization of pyrazines
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Glycogen synthase kinase-3β, also called tau phosphorylating kinase, is a proline-directed serine/threonine kinase which was originally identified due to its role in glycogen metabolism. Active forms of GSK3β localize to pretangle pathology including dystrophic neuritis and neurofibrillary tangles in Alzheimers disease (AD) brain. By using a high throughput screening (HTS) approach to search for new chemical series and cocrystallization of key analogues to guide the optimization and synthesis of our pyrazine series, we have developed highly potent and selective inhibitors showing cellular efficacy and bloo-brain barrier penetrance. The inhibitors are suitable for in vivo efficacy testing and may serve as a new treatment strategy for Alzheimers disease.
- Berg, Stefan,Bergh, Margareta,Hellberg, Sven,Hoegdin, Katharina,Lo-Alfredsson, Yvonne,Soederman, Peter,Von Berg, Stefan,Weigelt, Tatjana,Ormoe, Mats,Xue, Yafeng,Tucker, Julie,Neelissen, Jan,Jerning, Eva,Nilsson, Yvonne,Bhat, Ratan
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p. 9107 - 9119,13
(2020/10/15)
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- NEMATOCIDAL SULFONAMIDES
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Disclosed are compounds of Formula 1 (see "Formula 1"), N-oxides, and salts thereof, wherein Z is O or S; and R1, R2, R3, Q and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
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Page/Page column 57-58
(2010/11/18)
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