YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Synthesis and Antibacterial Activities of 3-[(4-Carboxy-3-hydroxyisothiazol-5-yl)thiomethyl] cephalosporin Derivatives

3-[(4-카르복시-3-히드록시이소티아졸-5-일)티오메틸] 세파로스포린 유도체들의 합성 및 항균력

  • 이영행 (원광대학교 자연과학대학 화학과) ;
  • 박규종 (원광대학교 자연과학대학 화학과) ;
  • 김하정 (순천향대학교 자연과학대학 생명과학부) ;
  • 최원식 (순천향대학교 자연과학대학 생명과학부)
  • Published : 1998.08.01
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Abstract

New cephalosporin antibiotics. 7-[(1H-tetrazolyl)acetamidol]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid trisodium salt 2,7-[(5-ethylthio-3-hydroxyisothiazol-4-yl)carbox-amidol-3-[(4-carboxy-3-hydroxyisothiazo1-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 3,7-[(2-aminothiazol-4-yl)acetamido]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl]thiomethyl]-3-cephem-4-caboxylic acid 4,7-[(Z)-2-(2-aminothiazol-4-yl)-2-(alkoxyimino)acetamido)-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 5-9 were synthesized. Antibacterial activities of these new cephalosporin derivatives and the relationship between their structures and activities were examined. Among them, 7-((Z)-2-(2-aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido)-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 8 and 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(l-carboxy-1-methylethoxyimino)acetamido]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 9 exhibited good antibacterial activities compared with those of cefotaxime and ceftriaxone.

Keywords

References

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