70671-46-4Relevant articles and documents
Synthesis of hydroxymethyl side-chained α-aminoxy diamide
Luo, Zheng,Yang, Hai-Feng,Chang, Xiao-Wei,Zhang, Dan-Wei
, p. 2815 - 2821 (2010)
Unnatural polar α-aminoxy acid residue with proteingenous hydroxymethyl side chain, a building block of the peptidomimetic foldamer of -aminoxy peptide, was synthesized starting from natural amino acid L-serine. The starting material, L-serine, undergoes a reaction sequence to produce compound 1 in three steps: (1) the neighboring carboxyl group participates in diazotization/bromination to transform the amino group to a bromo group, (2) the C-terminal carboxyl group is protected, and (3) bromide is SN2-displaced by N-hydroxyl phthalimide to introduce a N-O bond. After several conventional deprotection/coupling reactions, compound 1 is easily transformed to an -aminoxy diamide, which can be widely used in peptidomimetics design.
Quinoline derivative having indoleamine-2,3-dioxygenase inhibitory activity
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Paragraph 0442-0444, (2020/04/17)
The present invention provides a quinoline derivative having indoleamine-2,3-dioxygenase inhibitory activity, specifically a compound represented by a general formula (I) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition and a pr
Synthesis of Functionalized N-Acetyl Muramic Acids to Probe Bacterial Cell Wall Recycling and Biosynthesis
Demeester, Kristen E.,Liang, Hai,Jensen, Matthew R.,Jones, Zachary S.,D'Ambrosio, Elizabeth A.,Scinto, Samuel L.,Zhou, Junhui,Grimes, Catherine L.
supporting information, p. 9458 - 9465 (2018/07/21)
Uridine diphosphate N-acetyl muramic acid (UDP NAM) is a critical intermediate in bacterial peptidoglycan (PG) biosynthesis. As the primary source of muramic acid that shapes the PG backbone, modifications installed at the UDP NAM intermediate can be used to selectively tag and manipulate this polymer via metabolic incorporation. However, synthetic and purification strategies to access large quantities of these PG building blocks, as well as their derivatives, are challenging. A robust chemoenzymatic synthesis was developed using an expanded NAM library to produce a variety of 2-N-functionalized UDP NAMs. In addition, a synthetic strategy to access bio-orthogonal 3-lactic acid NAM derivatives was developed. The chemoenzymatic UDP synthesis revealed that the bacterial cell wall recycling enzymes MurNAc/GlcNAc anomeric kinase (AmgK) and NAM α-1 phosphate uridylyl transferase (MurU) were permissive to permutations at the two and three positions of the sugar donor. We further explored the utility of these derivatives in the fluorescent labeling of both Gram (-) and Gram (+) PG in whole cells using a variety of bio-orthogonal chemistries including the tetrazine ligation. This report allows for rapid and scalable access to a variety of functionalized NAMs and UDP NAMs, which now can be used in tandem with other complementary bio-orthogonal labeling strategies to address fundamental questions surrounding PG's role in immunology and microbiology.
NOVEL CYCLIC DEPSIPEPTIDE DERIVATIVES AND HARMFUL ORGANISM CONTROL AGENTS COMPRISING THE SAME
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Paragraph 0305; 0306; 0307; 0308, (2017/08/26)
An objective of the present invention is to provide novel cyclic depsipeptide derivatives and harmful organism control agents including the same as each other. Specifically, the present invention provides compounds represented by formula (1) or stereoisom