Design, synthesis and biological evaluation of glutamic acid derivatives as anti-oxidant and anti-inflammatory agents
A series of glutamic acid derivatives was synthesized and evaluated for their antioxidant activity and stability. We found several potent and stable glutamic acid derivatives. Among them, compound 12b exhibited good in vitro activity, chemical stability and cytotoxicity. A prototype compound 12b showed an anti-inflammatory effect in LPS-stimulated RAW 264.7 cell lines and in a zebrafish model.
Pagire, Suvarna H.,Lee, Eunhye,Pagire, Haushabhau S.,Bae, Eun Jung,Ryu, Soo Jung,Lee, Dahye,Kim, Min Hee,Kim, Geum Ran,Hwang, Kyu-Seok,Ahn, Sukyung,Maeng, Jin Hee,Song, Jin Sook,Bae, Myung Ae,Lee, Don Hang,Ahn, Jin Hee
p. 529 - 532
(2018/01/04)
Continuous-Flow Process for the Synthesis of 2-Ethylphenylhydrazine Hydrochloride
An expeditious process for the synthesis of 2-ethylphenylhydrazine hydrochloride via a continuous-flow reactor from 2-ethylaniline in 94% yield was described. The main steps in this synthesis involved not only the generation of diazonium salt intermediate in situ but also the temperature-programmed reduction by sodium sulfite in the tandem loop reactor. Total residence time was reduced to less than 31 min by increasing the reaction temperature and thereby taking advantage of improved mass and heat transfer of a continuous-flow system. The purification process was simplified by extraction of impurities in situ.
Synthesis, crystal structure and fungicidal activities of new type oxazolidinone-based strobilurin analogues
A series of oxazolidinone-based strobilurin analogues were efficiently synthesized by the reaction of 3-(2-bromomethylphenyl) oxazolidin-2-one with 1-substituted phenyl-2H-pyrazolin-3-one. Their structures were confirmed and characterized by 1H-NMR, 13C-NMR, elemental analysis, and mass spectroscopy. In addition, the crystal structure of the target compound 3-(2-((1-phenyl-2H-pyrazol-3-yloxy)methyl)phenyl) oxazolidin-2-one was determined by single crystal X-ray diffraction. The bioassay results of these compounds indicated that some of the oxazolidin-2-one derivatives containing N-substituted phenyl 2H-pyrazol ring exhibited potential in vivo fungicidal activities against M. grisea at the dosage of 1 g L-1.
Process for preparing 1,8-diethyl-1,3,4,9-tetrahydropyrano(3,4-b)-indole-1-acetic acid, etodolac
A process for preparing 1,8-diethyl-1,3,4,9-tetrahydro[3,4-b]-indole-1-acetic acid (etodolac) is disclosed. Etodolac is a useful antiinflammatory and analgesic agent.
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(2008/06/13)
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