- N-transfer reagent and method for preparing the same and its application
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Provided are a novel N-transfer reagent and a method for preparing the same and its application. The N-transfer reagent is represented by the following Formula (I): The various novel N-transfer reagents of the present invention can be quickly prepared by employing different nitrobenzene precursors. The N-transfer reagents can directly convert a variety of amino compounds into diazo compounds under mild conditions. Particularly, the N-transfer reagents can facilitate the synthesis of the diazo compounds. The application of synthesizing diazo compounds of the present invention can greatly decrease the difficulty in operation, increase the safety during experiments, reduce the cost of production and the environmental pollution, and enhance the industrial value of diazo compounds.
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- C1-Phostphonate Analogue of UDP-GlcNAc for Inhibition of O-GlcNAc Transferase
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A novel C1-phosphate analogue of uridine-5′-diphosphate (UDP)-GlcNAc as an effective OGT (O-linked N-acetylglucosamine (O-GlcNAc) transferase) inhibitor, and a preparation method for the same provides a compound having an OGT inhibitory effect that can be
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Paragraph 0032; 0033
(2017/02/24)
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- Synthesis of a benzene-containing C1-phosphonate analogue of UDP-GlcNAc for the inhibition of O-GlcNAc transferase
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I report here the design, synthesis, and biological evaluation of a new C1-phosphonate analogue of UDP-GlcNAc as a potential inhibitor of OGT, an enzyme responsible for O-GlcNAc modification. The analogue was designed to mimic the transition state of the
- Im, Jungkyun
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- Discovery and Structure-Activity Relationships of the Neoseptins: A New Class of Toll-like Receptor-4 (TLR4) Agonists
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Herein, we report studies leading to the discovery of the neoseptins and a comprehensive examination of the structure-activity relationships (SARs) of this new class of small-molecule mouse Toll-like receptor 4 (mTLR4) agonists. The compounds in this class, which emerged from screening an α-helix mimetic library, stimulate the immune response, act by a well-defined mechanism (mouse TLR4 agonist), are easy to produce and structurally manipulate, exhibit exquisite SARs, are nontoxic, and elicit improved and qualitatively different responses compared to lipopolysaccharide, even though they share the same receptor.
- Morin, Matthew D.,Wang, Ying,Jones, Brian T.,Su, Lijing,Surakattula, Murali M. R. P.,Berger, Michael,Huang, Hua,Beutler, Elliot K.,Zhang, Hong,Beutler, Bruce,Boger, Dale L.
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supporting information
p. 4812 - 4830
(2016/06/13)
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- NEOSEPTINS: SMALL MOLECULE ADJUVANTS
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A MD-2:TLR4 complex agonist compound is disclosed whose structure corresponds to Formula (I), as defined within. Also disclosed are a method of its preparation and use, as well as a pharmaceutical composition containing the same.
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Page/Page column 138
(2014/09/03)
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- O-nitrobenzyl photolabile protecting groups with red-shifted absorption: Syntheses and uncaging cross-sections for one- And two-photon excitation
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We evaluated the o-nitrobenzyl platform for designing photolabile protecting groups with red-shifted absorption that could be photolyzed upon one- and two-photon excitation. Several synthetic pathways to build different conjugated o-nitrobenzyl backbones,
- Aujard, Isabelle,Benbrahim, Chouaha,Gouget, Marine,Ruel, Odile,Baudin, Jean-Bernard,Neveu, Pierre,Jullien, Ludovic
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p. 6865 - 6879
(2007/10/03)
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