6078-46-2Relevant articles and documents
Preparation method of brain protective agent and key impurities thereof
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Paragraph 0023; 0038; 0042; 0046; 0047; 0054, (2021/07/08)
The invention relates to a preparation method of a brain protective agent and key impurities thereof. According to the invention, phenylhydrazine and ethyl acetoacetate serve as raw materials, edaravone and three key impurities of edaravone are synthesized in the same route, wherein the three key impurities include a transition-state impurity, edaravone dimer nitrogen oxide and 5-methyl-2-phenyl-4-(propyl-2-iene)-2,4-dihydro-3H-pyrazol-3-one; compared with respective synthesis of edaravone and each impurity, the method has the advantage that time and cost are saved; and experiments prove that the method of preparing edaravone by firstly controlling the process for synthesizing the transition-state impurities and then changing the process are higher in the yield and the purity of edaravone compared with direct synthesis of edaravone.
INDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
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Paragraph 0168-0171, (2013/10/22)
Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
Synthesis and biological evaluation of 5-aryloxypyrazole derivatives bearing a rhodanine-3-aromatic acid as potential antimicrobial agents
Zheng, Chang-Ji,Song, Ming-Xia,Sun, Liang-Peng,Wu, Yan,Hong, Lan,Piao, Hu-Ri
, p. 7024 - 7028 (2013/01/15)
Three novel series of 5-aryloxypyrazole derivatives have been synthesized and tested for their antibacterial activity. The majority of the synthesized compounds showed potent inhibitory activity against Gram-positive bacteria Staphylococcus aureus 4220, especially against the strains of multidrug-resistant clinical isolates (MRSA3167/3506 and QRSA3505/3519). Among which compounds IIIb, IIIg and IIIm showed the most potent levels of activity (MIC = 1 μg/mL) against the multidrug-resistant strains. And cytotoxic activity assay showed that the compounds tested did not affect cell viability on the Human cervical (HeLa) cells at their MICs. The current study therefore suggests that 5-aryloxypyrazoles bearing a rhodanine-3-aromatic acid moiety are promising scaffolds for the development of novel Gram-positive antibacterial agents.