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3-[(4-카르복시-5-에틸티오이소티아졸-3-일)옥시메틸] 세파로스포린 유도체들의 합성 및 항균력에 관한 연구
최원식(Won Sik Choi),박의석(Eui Suk Park),박규종(Kyu Jong Park),이영행(Young Haeng Lee) 대한약학회 2000 약학회지 Vol.44 No.2
New cephalosporin antibiotics, 3-[(4-carboxy-5-ethylthioisothiazol-3-yl)oxymethyll-7-[(1H-tetra-zol-1-yl)acetamido]-3-cephem-4-carboxylic acid 2, 3-[(4-carboxy-5-ethylthioisothiazol-3-yl)oxymethyl]-7-[(2-aminothiazol-4-yl)acetamidol-3-cephem-4-carboxylic acid 3, 3-[(4-carboxy-5-ethylthioisothiazol-3-yl)-oxymethyl]-7-[5-(ethylthio-3-hydroxyisothiazol-4-yl)carboxamido]-3-cephem-4-carboxylic acid 4, 3-[(4-carboxy-5-ethylthioisothiazol-3-yl)oxymethyl]-7-[(Z)-2-(fur-2-yl)-2-(methoxyimino)acetamido]-3-cephem-4-carboxylic acid 5, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-[(alkoxyimino)acetamido]-3-[(4-carboxy-5-ethylthioisothiazol-3-yl)oxymethyl]-3-cephem-4-carboxylic acid 6-8 were synthesized. Antibacterial activities and structure-activity relationships of these new cephalosporin derivatives were examined. Among them, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-l-methylethoxyimino)acetamido]-3-[(4-carboxy-5-ethylthylthioisothiazol-3-yl)oxymethyl]-3-cephem-4-carboxylic acid 7 exhibited good antibacterial activities compared to cefotaxime and ceftriaxone.
새로운 세파로스포린 유도체의 합성과 항균력에 관한 연구
박의석,김하정,최원식,황선암 순천향대학교 기초과학연구소 1996 순천향자연과학연구 논문집 Vol.2 No.1
New cephalosporin antibiotics, 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl 1-oxide) -acetamido]-3-heterocyclothiomethyl-3-cephem-4-carboxylic acid derivatives (2a-2d) were synthesized. Anti-bacterial activities of these new cephalosporin derivatives and the relationship between their stucture and their activities were examined. Among them, 7-[3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4- thiazin-3-yl1-oxide)acetamido]-3-[(2-methyl-1,3,4-thiadiazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid exhibited the broad antibacterial activities against Gram(+) and Gram(-) bacteria.