• 제목/요약/키워드: ACLE

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3-(치환) 피로리딘세파로스포린의 합성과 항균활성평가 (Synthesis and Antimicrobial Evaluation of 3-(Substituted) Pyrrolidine Cephalosporins)

  • 유지석;하재천;고옥현;유진철;강형룡
    • 약학회지
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    • 제43권3호
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    • pp.306-315
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    • 1999
  • To develop new cephalosporin antibiotics with improved antibacterial activities, a series of 7$\beta$-[2-(2-aminothiazol-4-y)-(Z)-2-(1-carboxy-1-methylethoxyimino)acetamido] -3-[5-(heterocycle)thiomethylpy-rrolidin-3-ylthio]methyl-3-cephem-4-carboxylic acid (14~18) having aminothiazol carboxymethylethoxy-imino 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.

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3- (치환) 테트라조일메칠세파로스포린의 합성과 생리활성 (Synthesis and Biological Activity of 3 - (Substituted) Tetrazolylmethyl Cephalosporins)

  • 고옥현;김영수;고봉석;이재영;하재천;방희재;유진철;강형룡
    • 약학회지
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    • 제42권1호
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    • pp.12-24
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    • 1998
  • For the development of new cephalosporin antibiotics with aminothiazolcarboxymethylethoxyimino moiety on the C-7 position and tetrazolymethyl moiety on the C-3 position of cephe m ring, 7${\beta}$-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[5-(substituted)tetrazol-2-yl]methyl-3-cephem-4-carboxylic acids(28-35) were synthesized. These compounds were tested for antimicrobial activity in vitro against Gram(+) and Gram(-) bacteria. They showed remarkable antibacterial activity against Escherichia coli AB 1157, Escherichia coli AB 0111, Escherichia coli BE 1186, Micrococcus luteus ATCC 9341, Salmonella typhimurium TV 119, Salmonella typhimurium SL 1102, Staphylococcus aureus IFO 12732, Staphylococcus aureus R-209, but these compounds were not active against Pseudomonas aeruginosa N-10.

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