Journal of the Korean Chemical Society (대한화학회지)

Korean Chemical Society (대한화학회)
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Studies on the Synthesis of New Medicinal Agent (Ⅲ) : Studies on the Synthesis and Antibacterial Activites of New Cephalosporin Derivatives

새로운 의약품의 합성에 관한 연구 (Ⅲ) : 새로운 세파로스포린 항생물질의 합성과 그의 생물활성에 관한 연구

  • 최원식 (순천향대학교 유전공학과) ;
  • 최소영 (순천향대학교 유전공학과)
  • Published : 19940800
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Abstract

New cephalosporin antibiotics,7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-[(substituted pyrimidin-2-yl)thiomethyl]-3-cephem-4-carboxylic acid derivatives(2a∼2d) were synthesized. These new cephalosporin derivatives were prepared by the introduction of pyridinylthiomethyl moiety in 3-position and thiazine group in 7-position of 7-ACA. Antibacterial activities of these compounds were examined and the relationship between structure and activities were studied. As the result, these compounds showed low antibacterial activities compared to cefotaxim used as control.

새로운 cephalosporin 항생물질인 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-[(substituted pyrimidin-2-yl)thiomethyl]-3-cephem-4-carboxylic acid derivatives(2a∼2d)유도체들을 합성하였다. 7-ACA의 3-위치에는 pyridinylthiomethyl기를 도입시키고, 7-위치에는 thiazine를 치환시켜서 구조 변화에 대한 항균 활성을 측정하였다. 그 결과 이들 유도체들은 기준물질인 cefotaxim보다 낮은 항균력을 나타내었다.

Keywords

References

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