- Bioorthogonal Click and Release Reaction of Iminosydnones with Cycloalkynes
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We report the discovery of a new bioorthogonal click-and-release reaction involving iminosydnones and strained alkynes. This transformation leads to two products resulting from the ligation and fragmentation of iminosydnones under physiological conditions. Optimized iminosydnones were successfully used to design innovative cleavable linkers for protein modification, thus opening up new areas in the fields of drug release and target-fishing applications. This click-and-release technology offers the possibility of exchanging tags on proteins for functionalized cyclooctynes under mild and bioorthogonal conditions.
- Bernard, Sabrina,Audisio, Davide,Riomet, Margaux,Bregant, Sarah,Sallustrau, Antoine,Plougastel, Lucie,Decuypere, Elodie,Gabillet, Sandra,Kumar, Ramar Arun,Elyian, Jijy,Trinh, Minh Nguyet,Koniev, Oleksandr,Wagner, Alain,Kolodych, Sergii,Taran, Frédéric
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supporting information
p. 15612 - 15616
(2017/12/02)
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- Synthesis and Physical Properties of First 3,3'-Bridged Bis- and Tris(1,3-thiazolium-4-olates) as well as of One 5,5'-Bridged Bis(1,3-thiazolium-4-olate) and its Conversion into 3,3'-(1,4-Phenylene)bis
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The synthesis and physical properties of the novel title compounds of type 7, 9, and 12, which contain two or in one case three mesoionic 1,3-thiazol-4-one systems, are described.With dimethyl acetylenedicarboxylate or dibenzoylethyne, 12 reacts under eli
- Gotthardt, Hans,Pflaumbaum, Wolfgang
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p. 1017 - 1022
(2007/10/02)
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- Antitrichomonal Activity of Mesoionic Thiazolopyridines
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Screening of mesoionic compounds as potential electron acceptors by analogy with metronidazole led to the finding of in vitro antitrichomonal activity for anhydro-2-phenyl-3-hydroxythiazolopyridinium hydroxide (1).In a series of analogues, potent i
- Walker, Keith A. M.,Sjogren, Eric B.,Matthews, Thomas R.
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p. 1673 - 1679
(2007/10/02)
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