3-(치환) 피로리딘세파로스포린의 합성과 항균활성평가

Synthesis and Antimicrobial Evaluation of 3-(Substituted) Pyrrolidine Cephalosporins

To develop new cephalosporin antibiotics with improved antibacterial activities, a series of 7beta-[2-(2-aminothiazol-4-yl)-(Z)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[5-(heterocycle)thiomethylpyrrolidin-3-ylthio]methyl-3-cephem-4-carboxylic acid (14-18) having aminothiazol carboxymethylethoxyimino group on the C-7 position and (heterocycle) thiomethyl pyrrolidinthiomethyl group on the C-3 position of the cephem ring were synthesized. These compounds were tested for antimicrobial activity in vitro against Gram(+) and Gram(-) bacteria. Compounds 15 and 16 showed remarkable antibacterial activity against Salmonella typhimurium TV119 and Alcalienes faecalis KCTC1004, but most of compounds showed lower activity than cefotaxime.