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- Bharate, Sandip B., et al.
(författare)
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Discovery of 7-(Prolinol-N-yl)-2-phenylamino-thiazolo[5,4-d]pyrimidines as Novel Non-Nucleoside Partial Agonists for the A(2A) Adenosine Receptor : Prediction from Molecular Modeling
- 2016
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Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 59:12, s. 5922-5928
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Tidskriftsartikel (refereegranskat)abstract
- We describe the identification of 7-(prolinol-N-yl)-2-phenylamino-thiazolo[5,4-d]pyrimidines as a novel chemotype of non-nucleoside partial agonists for the A(2A) adenosine receptor (A(2A)AR). Molecular-modeling indicated that the (S)-2-hydroxymethylene-pyrrolidine could mimic the interactions of agonists' ribose, suggesting that this class of compounds could have agonistic properties. This was confirmed by functional assays on the A(2A)AR, where their efficacy could be associated with the presence of the 2-hydroxymethylene moiety. Additionally, the best compound displays promising affinity, selectivity profile, and physicochemical properties.
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- Wang, Lei, et al.
(författare)
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Organic Polymer Dots as Photocatalysts for Visible Light-Driven Hydrogen Generation
- 2016
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Ingår i: Angewandte Chemie International Edition. - : Wiley. - 1433-7851 .- 1521-3773. ; 55:40, s. 12306-12310
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Tidskriftsartikel (refereegranskat)abstract
- For the first time, organic semiconducting polymer dots (Pdots) based on poly[(9,9'-dioctylfluorenyl-2,7-diyl)-co-(1,4-benzo-{2,1', 3} thiadiazole)] (PFBT) and polystyrene grafting with carboxyl-group-functionalized ethylene oxide (PS-PEG-COOH) are introduced as a photocatalyst towards visible-light-driven hydrogen generation in a completely organic solvent-free system. With these organic Pdots as the photocatalyst, an impressive initial rate constant of 8.3 mmol h(-1) g(-1) was obtained for visible-light-driven hydrogen production, which is 5-orders of magnitude higher than that of pristine PFBT polymer under the same catalytic conditions. Detailed kinetics studies suggest that the productive electron transfer quench of the excited state of Pdots by an electron donor is about 40%. More importantly, we also found that the Pdots can tolerate oxygen during catalysis, which is crucial for further application of this material for light-driven water splitting.
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