The Experts below are selected from a list of 2544 Experts worldwide ranked by ideXlab platform
Pierre-yves Renard - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and reactivity of a bis-Sultone cross-linker for peptide conjugation and [18F]-radiolabelling via unusual "double click" approach.
Organic and Biomolecular Chemistry, 2012Co-Authors: Thomas Priem, Cédric Bouteiller, David Camporese, Anthony Romieu, Pierre-yves RenardAbstract:A novel homobifunctional cross-linker based on a bis-Sultone benzenic scaffold was synthesised. The potential utility of this bioconjugation reagent was demonstrated through the preparation of an original prosthetic group suitable for the [(18)F]-labelling of peptides. The labelling strategy is based on the nucleophilic fluorination via the ring-opening of a first Sultone moiety followed by the nucleophilic ring-opening of the second remanent Sultone by a reactive amine of the biopolymer. Beyond the one-step radiolabelling of the peptide, the second main advantage of this strategy is the release of free sulfonic acid moieties making the separation of the targeted [(18)F]-tagged sulfonated compound from its non-sulfonated precursor easier and thus faster. This first report of the successful use of a bis-Sultone moiety as a versatile bioconjugatable group was demonstrated through a comprehensive reactivity study involving various nucleophiles, especially those commonly found in biopolymers. An illustrative example, highlighting the potential of this unusual and promising "double click" conjugation approach, was devoted to the radiolabelling of a biological relevant peptide.
Thomas Priem - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and reactivity of a bis-Sultone cross-linker for peptide conjugation and [18F]-radiolabelling via unusual "double click" approach.
Organic and Biomolecular Chemistry, 2012Co-Authors: Thomas Priem, Cédric Bouteiller, David Camporese, Anthony Romieu, Pierre-yves RenardAbstract:A novel homobifunctional cross-linker based on a bis-Sultone benzenic scaffold was synthesised. The potential utility of this bioconjugation reagent was demonstrated through the preparation of an original prosthetic group suitable for the [(18)F]-labelling of peptides. The labelling strategy is based on the nucleophilic fluorination via the ring-opening of a first Sultone moiety followed by the nucleophilic ring-opening of the second remanent Sultone by a reactive amine of the biopolymer. Beyond the one-step radiolabelling of the peptide, the second main advantage of this strategy is the release of free sulfonic acid moieties making the separation of the targeted [(18)F]-tagged sulfonated compound from its non-sulfonated precursor easier and thus faster. This first report of the successful use of a bis-Sultone moiety as a versatile bioconjugatable group was demonstrated through a comprehensive reactivity study involving various nucleophiles, especially those commonly found in biopolymers. An illustrative example, highlighting the potential of this unusual and promising "double click" conjugation approach, was devoted to the radiolabelling of a biological relevant peptide.
Haimin Lei - One of the best experts on this subject based on the ideXlab platform.
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new synthesis method for Sultone derivatives synthesis crystal structure and biological evaluation of s ca
Molecules, 2015Co-Authors: Wenqiang Yan, Chenze Zhang, Yuzhong Zhang, Miao Liang, Fuhao Chu, Yan Gong, Penglong Wang, Haimin LeiAbstract:There has been no remarkable progress in the synthesis of Sultones in recent years. To facilitate more detailed studies of this functional group, we found a new method to synthesize the sulfonic acid lactone derivatives and finish its ring-closing reaction. A new Sultone derivative, (E)-ethyl 4-oxo-6-styryl-3,4-dihydro-1,2-oxathiine-5-carboxylate 2,2-dioxide (S-CA), was synthesized and structurally identified by 1H-NMR, 13C-NMR, HMQC and X-ray single crystal diffraction analysis. The new rapid synthesis extended the method of ring-closing reaction of sulfonic acid lactone derivatives. The angiogenesis activities of S-CA were evaluated by the chick chorioallantoic membrane (CAM) model. It could selectively suppress small angiogenesis in CAM, without influencing either middle and large angiogenesis. In addition, anticancer efficacy of S-CA was evaluated in vivo using a murine sarcoma S180 model. Reduction of the tumor weight and tumor HE staining regions demonstrated that S-CA (10 mg/kg, intraperitoneal injection) had potent inhibition effects and a 44.71% inhibitory rate in S180 mice. Moreover, an acute toxicity test showed that the LD50 value of S-CA via intraperitoneal injection was 25.624 mg/kg.
Youyi Xu - One of the best experts on this subject based on the ideXlab platform.
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enhancing the antifouling and antimicrobial properties of poly ether sulfone membranes by surface quaternization from a reactive poly ether sulfone based copolymer additive
Industrial & Engineering Chemistry Research, 2014Co-Authors: Yifan Zhao, Jinhong Jiang, Zhuan Yi, Youyi XuAbstract:A facile and practical method for fabricating antifouling and antimicrobial poly(ether sulfone) (PES) membranes is developed in this work. A PES blend membrane was first fabricated by a traditional nonsolvent induced phase separation (NIPS) process with a reactive amphiphilic copolymer poly(ether sulfone)-block-poly(2-(dimethylamino) ethyl methacrylate) (PDMAEMA-b-PES-b-PDMAEMA) as the blending additive. The hydrophilic PDMAEMA chains in the copolymer additive spontaneously migrated toward the interfaces between membrane and coagulant bath (usually water) during membrane formation. The enriched PDMAEMA chains on the as-made blend membranes were then quaternized by reacting with 1,3-propane Sultone (1,3-PS) and 1-bromodecane, respectively. The zwitterionic PES membranes obtained from 1,3-PS treatment showed significantly improved antifouling ability and hemocompatibility. In another case, the resulting cationic PES membranes treated with 1-bromodecane exhibited excellent antibacterial activities against Es...
Sudarshan Debnath - One of the best experts on this subject based on the ideXlab platform.
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synthesis of uracil coumarin and quinolone fused benzosultams and benzoSultones
Synthesis, 2015Co-Authors: Shovan Mondal, Sudarshan DebnathAbstract:An efficient method for the regioselective synthesis of uracil-, coumarin- and quinolone-fused benzosultams and benzoSultones is reported. The method offers a synthetic route to highly functionalized sultam and Sultone derivatives in 75–95% yield under mild conditions. Density functional theory studies have been used to explain the regioselectivity in the synthesis of the coumarin- and quinolone-fused sultams and Sultones.
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Synthesis of seven-membered fused Sultones by reductive Heck cyclization: an investigation for stereochemistry through DFT study
Tetrahedron, 2015Co-Authors: Shovan Mondal, Sudarshan DebnathAbstract:Abstract An efficient method for the synthesis of seven-membered fused Sultones via Pd(0) catalyzed intramolecular reductive Heck cyclization is reported. The method offers the regio- and stereoselective synthesis of highly functionalized benzopyrido-fused or dibenzo-fused Sultone derivatives in 80–95% yield under mild conditions. Chemoselective Sonogashira coupling is utilized for the synthesis of cyclization precursors. The stereochemistry of the exocyclic double bond of Sultone derivatives is confirmed from single crystal X-ray diffraction. The stereochemistry of the exocyclic double bond in dibenzo-fused Sultones is reverse with reference to that of benzopyrido-fused Sultones due to the presence of an interaction between the lone pair of nitrogen in pyridine with the electron deficient Pd(II). This interaction is confirmed through DFT (density functional theory) studies. The mechanistic role of water is established through deuterium exchange reaction.
