The title compound N-[1-(4-chlorophenyl)-1,4-dihydro-4-oxe-6-methylpyridazine- 3-carbonyl]-N(-benzoylhydrazine was prepared by the reaction of 1-(4-chlorophenyl)-1,4- dihydro-4-oxe-6-methylpyridazine-3-carboxylic acid...The title compound N-[1-(4-chlorophenyl)-1,4-dihydro-4-oxe-6-methylpyridazine- 3-carbonyl]-N(-benzoylhydrazine was prepared by the reaction of 1-(4-chlorophenyl)-1,4- dihydro-4-oxe-6-methylpyridazine-3-carboxylic acid with chloroformate ethyl ester and benzoyl hydrazine in the presence of triethylamine. The crystal structure ([C19H15ClN4O3]2·C2H5OH, Mr =811.67) has been determined by X-ray crystal structural analysis. The crystal is monoclinic, space group P21/c, with unit cell parameters a=13.296(3), b=17.155(3), c=17.459(3)?,β=98.959(4), Z=4, V=3934(1) ?3, Dc=1.371g/cm3, F(000)=1688, μ(MoKα)=0.226 mm-1, R=0.0495, wR=0.1348 for 3345 observed reflections (I >2σ(I)). The hydrogen bonds N(3)－H…O(1) , N(7)－H…O(4), and N(8)－H…O(2) can be observed.展开更多
N-acetyl-glucosamine, the monomer of chitin, was cyclo-condensed with L-cysteine to prepare thiazolidine derivative： 2-N-acetyl-glucosamine-thiazolidine-4（R）-carboxylic acid （GlcNAcCys）. The stability of GlcNAcCy...N-acetyl-glucosamine, the monomer of chitin, was cyclo-condensed with L-cysteine to prepare thiazolidine derivative： 2-N-acetyl-glucosamine-thiazolidine-4（R）-carboxylic acid （GlcNAcCys）. The stability of GlcNAcCys was evaluated by high performance liquid chromatography （HPLC） measurement. The results showed that GlcNAcCys was more stable than other TCA derivatives, especially in alkaline condition. The direct in vitro antioxidative properties of GlcNAcCys were investigated by using UV radiation-induced lipid peroxidation （LPO） in mitochondria and nuclei and . OH-induced LPO in red blood cell （RBC） ghosts models. UV radiation caused dose-dependent LPO in both mitochondria and nuclei. This effect was catalyzed by addition of Fe^2 ＋ while prevented by co-incubation with GlcNAcCys. When nuclei and mitochondria was treated with 100μl, 300μl, 500μl of GlcNAcCys and co-incubated at 37℃ for 30min, LPO was decreased to 96%, 72%, 68% in nuclei and 95%, 72%, 68% in mitochondria when compared to the UV radiation group respectively. Hydroxyl radicals （. OH） generated by Fenton reaction induced LPO in RBC ghosts. Pretreatment of RBC ghosts with GlcNAcCys could induce antioxidant RBC ghosts and inhibit concentration-dependent malondialdehyde （MDA） formation in antioxidant RBC ghosts. Its inhibition percent was 14%, 35%, 36%, 42% at 10, 20, 30, 40mg/ml respectively. In a conclusion, the data suggest that GlcNAcCys has antioxidant ability and can significantly inhibit lipid peroxidation in biological samples tested in vitro.展开更多
基金the National Nature Science Foundation (29832050).
文摘The title compound N-[1-(4-chlorophenyl)-1,4-dihydro-4-oxe-6-methylpyridazine- 3-carbonyl]-N(-benzoylhydrazine was prepared by the reaction of 1-(4-chlorophenyl)-1,4- dihydro-4-oxe-6-methylpyridazine-3-carboxylic acid with chloroformate ethyl ester and benzoyl hydrazine in the presence of triethylamine. The crystal structure ([C19H15ClN4O3]2·C2H5OH, Mr =811.67) has been determined by X-ray crystal structural analysis. The crystal is monoclinic, space group P21/c, with unit cell parameters a=13.296(3), b=17.155(3), c=17.459(3)?,β=98.959(4), Z=4, V=3934(1) ?3, Dc=1.371g/cm3, F(000)=1688, μ(MoKα)=0.226 mm-1, R=0.0495, wR=0.1348 for 3345 observed reflections (I >2σ(I)). The hydrogen bonds N(3)－H…O(1) , N(7)－H…O(4), and N(8)－H…O(2) can be observed.
文摘N-acetyl-glucosamine, the monomer of chitin, was cyclo-condensed with L-cysteine to prepare thiazolidine derivative： 2-N-acetyl-glucosamine-thiazolidine-4（R）-carboxylic acid （GlcNAcCys）. The stability of GlcNAcCys was evaluated by high performance liquid chromatography （HPLC） measurement. The results showed that GlcNAcCys was more stable than other TCA derivatives, especially in alkaline condition. The direct in vitro antioxidative properties of GlcNAcCys were investigated by using UV radiation-induced lipid peroxidation （LPO） in mitochondria and nuclei and . OH-induced LPO in red blood cell （RBC） ghosts models. UV radiation caused dose-dependent LPO in both mitochondria and nuclei. This effect was catalyzed by addition of Fe^2 ＋ while prevented by co-incubation with GlcNAcCys. When nuclei and mitochondria was treated with 100μl, 300μl, 500μl of GlcNAcCys and co-incubated at 37℃ for 30min, LPO was decreased to 96%, 72%, 68% in nuclei and 95%, 72%, 68% in mitochondria when compared to the UV radiation group respectively. Hydroxyl radicals （. OH） generated by Fenton reaction induced LPO in RBC ghosts. Pretreatment of RBC ghosts with GlcNAcCys could induce antioxidant RBC ghosts and inhibit concentration-dependent malondialdehyde （MDA） formation in antioxidant RBC ghosts. Its inhibition percent was 14%, 35%, 36%, 42% at 10, 20, 30, 40mg/ml respectively. In a conclusion, the data suggest that GlcNAcCys has antioxidant ability and can significantly inhibit lipid peroxidation in biological samples tested in vitro.
