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Phenazine dioxide 유도체가 간 Xanthine Oxidase 활성에 미치는 영향
강일영(Il Young Kang),김상렬(Sang Yul Kim),김호식(Ho Shik Kim),허근(Keun Huh) 대한약학회 1990 약학회지 Vol.34 No.2
8-Acyl-2-hydroxyphenzaine-5,10-dioxides and 8-acyl-2-aminophenazine-5,10-dioxides bearing n-butanoyl, n-hexanoyl and n-octanoyl groups were synthesized. It was attempted to observe the effect of phenazine dioxide derivatives on the hepatic xanthine oxidase activity in this study. As the activity of xanthine oxidase, the key enzyme in the generation of superoxide anion radical (O2), was measured in the presence of phenazine dioxide derivatives, the action of 8-acyl-2-hydroxyphenazine-5,10-dioxide derivatives inhibited with increase of numbers of carbon atom bearing 8-acyl group. Moreover, when plotted on double reciprocal form, the Vmax value decrease as increase of numbers of carbon atom bearing acyl groups without affecting the Km value. However, the hepatic xanthine oxidase activity was not changed by 8-acyl-2-aminophenazine-5,10-dioxide derivatives.
Phenazine dioxide 유도체가 간 Xanthine Oxidase 활성에 미치는 영향
강일영,김상렬,허근,김호식 영남대학교 약품개발연구소 1991 영남대학교 약품개발연구소 연구업적집 Vol.1 No.-
8-Acyl-2-hydroxyphenzaine-5, 10-dioxides and 8-acyl-2-aminophenazine-5, 10-dioxides bearing n-butanoyl, n-hexanoyl and n-octanoyl groups were synthesized. It was attempted to observe the effect of phenazine dioxide derivatives on the hepatic xanthine oxidase activity in this study. As the activity of xanthine oxidase, the key enzyme in the generation of superoxide anion radical (O₂^(-)), was measured in the presence of phenazine dioxide derivatives, the action of 8-acyl-2-hydroxyphenazine-5, 10-dioxide derivatives inhibited with increase of numbers of carbon atom bearing 8-acyl group. Moreover, when plotted on double reciprocal form, the Vmax value decrease as increase of numbers of carbon atom bearing acyl groups without affecting the Km value. However, the hepatic xanthine oxidase activity was not changed by 8-acyl-2-aminophenazine-5, 10-dioxide derivatives.
페나진 유도체의 합성과 항균성에 관한 연구(제 2 보)
姜一英,金相烈,金浩植,金鍾大,허근 영남대학교 약품개발연구소 1991 영남대학교 약품개발연구소 연구업적집 Vol.1 No.-
아세트아닐리드와 부타노일, 헥사노일, 옥타노일기를 가진 n-acyl chloride류로부터 6-acylbenzofuroxan류를 합성하고, 이들과 히드로퀴논 및 4-아미노페놀을 반응시켜 8-acyl-2-hydroxy-phenazine-5, 10-dioxide류와 8-acyl-2-aminophenazine-5, 10-dioxide류를 합성하였다. 이들 phenazine dioxide 유도체의 항균성을 희석법에 의하여 최소 발육저지 농도로서 조사하였는데, 그람양성균에서 옥타노일기를 가진 phenazine dioxide 유도체들이 부타노일기나 헥사노일기를 가진 유도체를 보다 항균성이 더 강하였으나, 그람음성균에서는 항균성과 아실기의 탄소수와는 관계가 없다는 것은 알았다. 활성산소(O₂-) 생성의 주효소인 xanthine oxidase의 활성을 phenazine dioxide 유도체 존재하에서 측정했을 때 8-acyl-2-hydroxyphenazine-5, 10-dioxide류의 효소활성 저해작용은 아실기의 탄소수가 증가함에 따라 증가하였다. 8-Acyl-2-hydroxyphenazine-5, 10-dioxides and 8-acyl-2-aminophenazine-5, 10-dioxides were synthesized by the reaction of hydroquinone and 4-aminophenol with 6-acyl-benzofuroxans which had been obtained from acetanilide and n-acyl chlorides bearing butanoyl, hexanoyl and octanoyl groups. The antimicrobial activities of these phenazine dioxide derivatives were investigated in terms of minimum inhibitory concentration by the common twofold dilution technique. It was observed that the antimicrobial activity of the phenazine dioxide derivatives bearing octanoyl group was stronger than that of those bearing butanoyl and hexanoyl groups in gram positive microorganisms, but it was observed that the antimicrobial activity and the number of the carbon atom of acyl groups did not have any relation in gram negative microorganisms. When the activity of xanthine oxidase which is the key enzyme in the generation of superoxide anion radical (O₂^(-)), was measured in the presence of phenazine dioxide derivatives, the inhibitory action of the enzyme activity of 8-acyl-2-hydroxyphenazine-5, 10-dioxides was increased in accordance with the number of the carbon atom of acyl groups.
金榮지,權五陳,姜一英 영남이공대학 1991 論文集 Vol.20 No.-
Butylated hydroxyanisole(BHA), butylated hydroxytoluene(BHT), tertiary butyihydroquinone (TBHQ) and propyl gullate(PG) at 0, 50, 100. 150, 200. 250, 300, 350, 400. 450 and 5II0pPm and selected combinations at 0, 100. 200, 300 and 400ppm in nutrient agar(solid system) and in brain heart infusion(liquid system) were tested for antibacterial activity on five gram negative and seven gram positive bacteria. The BHA and TBHQ were more effective than BHT and PG, respectively. Of the six combinations tested, the Bl IA-'PB1IQ combination inhibited the greatest number of organisms followed by BHA-BHT, BHA-PG, BHT-TBHQ, BHT-PG and TBHQ-PG, respectively. In general, the antioxidants inhibited grain positive bacteria, especially Sirepronryces gritees. more than gram negative bacteria. The antioxidants were more effective in nutrient agar than in brain heart infusion.
Isoxazolo [2,3-α]quinoxaline과 Pyrrolo [1,2-α]quinoxaline의 선택적인 합성에 관한 연구
金浩植,南順花,都理香,姜一英 대구효성가톨릭대학교 자연과학연구소 1989 基礎科學硏究論集 Vol.3 No.-
The reaction of 2,6-dichloroquinoxaline with m-chloroperbenzoic acid gave 2,6-dichloroqui-noxaline 4-oxide,whose reation with 4-butylaniline provided 2-substituted 6-chloroquinoxa-line 4-oxide. The isoxazolo( 2,3-α)quinoxaline and pyrrolo[ 1,2-α1 quinoxaline were selectively synthesized from the 2-substituted 6-chloroquinoxaline 4-oxide and dimethyl acetylenedicar-boxylate. Moreover, the pyrrolo( 1,2- α)quinoxaline was found to be produced by the ring transformation of the isoxazolo( 2,3- α)quinoxaline. A postulated reaction mechanism for the ring transformation of isoxazolo(2,3- α )quinoxaline into pyrrolo( 1,2-α) quinoxaline was prese-nted.
새로운 1-Aryl-3-quinoxalinyl-1,2,4-triazole 유도체의 합성에 관한 연구
김호식,도이향,남순화,강일영,박태주 대구효성가톨릭대학교 자연과학연구소 1990 基礎科學硏究論集 Vol.4 No.-
The reaction of 3-methoxycarbonylmethylene-2-oxo-1,2,3,4-tetrahydroquinoxaline with p-butylbenzenediazonium chloride gave α-arylhydrazonoester , whose reaction with hydra-zine hydrate afforded α -arylhydrazonoacylhydrazide . The reaction of α-aryl hyd razonoacylh-ydrazide with sodium nitrite in aqueous acetic acid provided a-arylhydrazonoacylazide and then its refluxing in N , N - dimethylformamide furnished 1-aryl-3-quinoxalinyl-1,2,4-triazole .
새로운 Pyrazole類의 合成에 관한 硏究 : 第1報 Ⅰ
南順花,李萬佶,郭美玉,姜一英,金浩植 대구효성가톨릭대학교 자연과학연구소 1991 基礎科學硏究論集 Vol.5 No.-
AbstrBct The reaction of 6-chloro-2- hydrazinoquinoxalines with acetylacetone or diben-zoylmethane gave pyrazoles via dehydration of the intermediate hydrazone and no triazolocompound was obtained. The probable mechanism for the formation of the pyrazole isdiscussed.
새로운 3-(α-Arylhydrazono)oxadiazolylmethyl-2-oxo-1 2-dihydroquinoxaline 誘導體의 合成과 토오토메리 現象에 관한 硏究
都理香,南順花,郭美玉,朴胎晝,姜一英,金浩植 대구효성가톨릭대학교 자연과학연구소 1991 基礎科學硏究論集 Vol.5 No.-
Abstract The reaction of 3-methoxycarbonylmethylene-2-oxo-1, 2, 3, 4-tetrahydro-quinoxaline with p-butylbenzenediazonium chloride gave n-arylhydrazonoester, whose reaction with hydrazine hydrate afforded α-arylhydrazonoacylhydrazide. The reaction of α-arylhydrazonoacylhydrazide with triethyl orthoformate resulted in the intramolecu-lar cyclization to give the 3-(α-(p-butylphenylhydrazono)-1,3,4-oxadiazol-2-ylmethyl)-2-oxo-1,2-dihydroquinoxaline, but not the 1, 2, 4, 5-tetrazepinylquinoxaline. The tautomericbehavior of 3-[α-(p-butylphenylhydrazono) methoxycarbonylmethyl]-2-oxo-1, 2-dihy-droquinoxaline and 3-[α-(p-butylphe nylhydrazono)-1, 3, 4- oxadiazol -2- ylmethyl ]-2-oxo-1,2-dihydroquinoxaline between the hydrazone imine and diazenyl enamine forms in the dimethyl sulfoxide solution was investigated on the basis of the tautomer ratio determined by the 1H-NMR spectral data.