518342-58-0Relevant academic research and scientific papers
LpxC Inhibitors: Design, Synthesis, and Biological Evaluation of Oxazolidinones as Gram-negative Antibacterial Agents
Kurasaki, Haruaki,Tsuda, Kosuke,Shinoyama, Mariko,Takaya, Noriko,Yamaguchi, Yuko,Kishii, Ryuta,Iwase, Kazuhiko,Ando, Naoki,Nomura, Masahiro,Kohno, Yasushi
, p. 623 - 628 (2016)
Herein we report a scaffold-hopping approach to identify a new scaffold with a zinc binding headgroup. Structural information was used to give novel oxazolidinone-based LpxC inhibitors. In particular, the most potent compound, 23j, showed a low efflux ratio, nanomolar potencies against E. coli LpxC enzyme, and excellent antibacterial activity against E. coli and K. pneumoniae. Computational docking was used to predict the interaction between 23j and E. coli LpxC, suggesting that the interactions with C207 and C63 contribute to the strong activity. These results provide new insights into the design of next-generation LpxC inhibitors.
Liquid crystal compound containing butadiyne structure and liquid crystal composition and application thereof
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Paragraph 0090; 0095-0097, (2021/05/08)
The invention relates to a liquid crystal compound containing a butadiyne structure. The liquid crystal compound is represented by a general formula I. The invention also relates to a liquid crystal composition which at least comprises the compound repres
HETEROCYCLIC COMPOUNDS AND USE THEREOF AS MODULATORS OF TYPE III RECEPTOR TYROSINE KINASES
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Paragraph 0445, (2016/08/03)
Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFRβ kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
DIPHENYLAMINO KETONE DERIVATIVES AS MEK INHIBITORS
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Page/Page column 17, (2010/02/10)
The present invention relates to diphenylamino ketone derivatives, pharmaceutical compositions and methods of use thereof.
N-(4-substituted phenyl)-anthranilic acid hydroxamate esters
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Page 21, (2010/02/05)
The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.
MEK INHIBITING OXA- AND THIA-DIAZOL-2-YL PHENYLAMINE DERIVATES
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Page 54, (2010/02/07)
This invention provides substituted Phenyl-(2-[1,3,4]thiadiazol-2-yl-phenyl)-amine and (2-[1,3,4]Oxadiazol-2-yl-phenyl)phenyl-amine compounds which act as inhibitors of MAPKIERK Kinase ("MEK") enzymes and pharmaceutical compositions and methods for their use in immunomodulation and in the treatment and alleviation of inflammation, and proliferative diseases such as cancer and restenosis.
Combinatorial synthesis of oligo(phenylene ethynylene)s
Hwang, Jiunn-Jye,Tour, James M.
, p. 10387 - 10405 (2007/10/03)
The combinatorial synthesis of oligo(phenylene ethynylene) tetramers, both in solution and on solid support, is described. These products are of interest for molecular electronics applications. An iterative sequence, coupling of aryl halides to alkynes under Sonogashira conditions, was used. Five monomers functionalized with electron-donating or electron-withdrawing groups were synthesized, and used to generate a library of 25 trimers in a solution-phase based process. A library of 24 tetramers was prepared by subsequent protodesilylation and coupling with the alligator clip 4-iodo-1-thioacetylbenzene. The solution-phase based sequence was successfully adapted to a higher yielding directed split-and-pool solid-phase process, with average yields of 78-86% for each step over seven steps. A triazene linker group was used to attach the starting monomer to the polymer beads. At the completion of the solid-phase-based process, traceless cleavage of trimers from the resin was achieved by sonication of the resin in 10% HCl/THF solution. The released products were then poised for the final step in the sequence, attachment of the alligator clip.
