3-[(4-카르복시-5-에틸티오이소티아졸-3-일)옥시메틸] 세파로스포린 유도체들의 합성 및 항균력에 관한 연구

A Study on the Synthesis and Antibacterial Activities of 3-[(4-Carboxy-5-ethylthioisothiazol-3-yl)oxymethyl] cephalosporin Derivatives

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.