- Design, synthesis and biological evaluation of glutamic acid derivatives as anti-oxidant and anti-inflammatory agents
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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
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- Drug Latentiation by γ-Glutamyl Transpeptidase
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The N-γ-glutamyl derivatives of L-thiazolidine-4-carboxylic acid, 4-aminobutyric acid, 1-aminocyclopentanecarboxylic acid, 2-aminophenol, and p-fluoro-L-phenylalanine (compounds 6, 8, 9, 10, and 12 respectively) were synthesized using the synthom phthaloylglutamic anhydride.Their relative rates of cleavage by the enzyme γ-glutamyl transpeptidase (γ-GT) were determined in order to evaluate the possibility for their selective release by this enzyme which is elevated in certain pathological conditions.Compounds 6, 8, and 9 were not readily solvolyzed by γ-GT, but compounds 10 and 12, as well as the N-γ-glutamylated derivatives of 3- and 4-aminophenol, were readily cleaved.
- Magnan, Sanne D. J.,Shirota, Frances N.,Nagasawa, Herbert T.
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p. 1018 - 1021
(2007/10/02)
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