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Analgesic and Antiinflammatory Activities of Some New Mannich Bases of 5-Nitro-2-Benzoxazolinones
Koksal, Meric,Kupeli, Esra,Yesilada, Erdem,Erdogan, Hakki,Gokhan, Mesrin 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.4
In this study, the synthesis of a novel series Mannich bases of 5-nitro-3-substituted piperazino-methyl-2-benzoxazolinones are described. The structures attributed to compounds 3a-3k were elucidated using IR, $^1$H-NMR spectroscopic techniques besides elemental analysis. The compounds were examined for their in vivo antiinflammatory and analgesic activities in two different bioassays, namely, carrageenan-induced hind paw edema and p-benzoquinone-inducedabdominal constriction tests in mice, respectively. In addition, the ulcerogenic effects of the compounds were determined. Among the tested derivatives most promising results were obtained for the compounds bearing electron-withdrawing substituents (F, Cl, COCH$_3$) in the ortho/para position of the phenyl nucleus on the piperazine ring at 3 position of benzoxazoli-none moiety (3a, 3b, 3c, 3d, 3h). The analgesic activities of all compounds are higher than their antiinflammatory activities. Antiinflammatory inhibitory ratios for all compounds were above 30% for the last two measurements. Because of this compounds 3a,3b,3c,3d deserve attention and may be considered for further evaluation.
Sukuroglu, Murat,Caliskanergun, Burcu,Unlu, Serdar,Sahin, M.Fethi,Kupeli, Esra,Yesilada, Erdem,Banoglu, Erden The Pharmaceutical Society of Korea 2005 Archives of Pharmacal Research Vol.28 No.5
A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4- chloro-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analygesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.
Mustafa Aslan,Didem Deliorman Orhan,Nil?fer Orhan,Ekrem Sezik,Erdem Yesilada 한국식품영양과학회 2007 Journal of medicinal food Vol.10 No.2
Helichrysum graveolens(Bieb.) Sweet (Asteraceae) grows widely in Turkey. Capitulums of H. graveolensareused in the treatment of many diseases such as jaundice and wound healing and as a diuretic in the rural areas of Anatolia.The decoction from the capitulums of the plant is consumed for the symptoms of diabetes mellitus in folk medicine. In thepresent study, the hypoglycemic, antihyperglycemic, and antioxidant potentials of water and ethanol extracts of H. graveolenswere evaluated by using in vivomethods in normal and streptozotocin-induced diabetic rats. Blood glucose levels of animalswere measured by the glucose oxidase method. The antioxidant activity of these extracts was also studied in liver, kidney,and heart tissues. In order to determine antioxidant activity, tissue malondialdehyde and reduced glutathione levels were mea-sured by using spectrophotometric methods. The experimental data obtained from water and ethanol extracts of capitulumsconfirmed the folkloric utilization. In order to discuss the role of polyphenolic components in the relevant activity, total phe-nol and flavonoid contents of each extract were also determined using the Folin-Ciocalteu reagent, and a positive correlationwas observed.
Analgesic and Antiinflammatory Activities of Some New Mannich Bases of 5-Nitro- 2-Benzoxazolinones
Meri?K?sal,Nesrin G?han,Esra K?eli,Erdem Yesilada,Hakki Erdogan 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.4
In this study, the synthesis of a novel series Mannich bases of 5-nitro-3-substituted piperazinomethyl- 2-benzoxazolinones are described. The structures attributed to compounds 3a-3k were elucidated using IR, 1H-NMR spectroscopic techniques besides elemental analysis. The compounds were examined for their in vivo antiinflammatory and analgesic activities in two different bioassays, namely, carrageenan-induced hind paw edema and p-benzoquinone-induced abdominal constriction tests in mice, respectively. In addition, the ulcerogenic effects of the compounds were determined. Among the tested derivatives most promising results were obtained for the compounds bearing electron-withdrawing substituents (F, Cl, COCH3) in the ortho/para position of the phenyl nucleus on the piperazine ring at 3 position of benzoxazolinone moiety (3a, 3b, 3c, 3d, 3h). The analgesic activities of all compounds are higher than their antiinflammatory activities. Antiinflammatory inhibitory ratios for all compounds were above 30% for the last two measurements. Because of this compounds 3a, 3b, 3c, 3d deserve attention and may be considered for further evaluation.
Murat SÜKÜROGLU,Burcu ÇALISKAN ERGÜN,Serdar ?L?,M. Fethi SAHIN,Esra K?ELI,Erdem YESILADA,Erden BANOGLU 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.5
A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4-chloro-pyrazole-1-yl)- 3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenaninduced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analgesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.