Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Synthesis and Physicochemical Studies on a Novel Cephalosporin, DWC-751

신규 세파로스포린 항생제 DWC-751 합성과 물성연구

  • 김명구 ((주)대웅제약 중앙연구소) ;
  • 안상근 ((주)대웅제약 중앙연구소) ;
  • 최영기 ((주)대웅제약 중앙연구소) ;
  • 문치장 ((주)대웅제약 중앙연구소) ;
  • 오세한 ((주)대웅제약 중앙연구소) ;
  • 성무제 ((주)대웅제약 중앙연구소) ;
  • 윤길중 ((주)대웅제약 중앙연구소) ;
  • 신종만 ((주)대웅제약 중앙연구소) ;
  • 김학형 ((주)대웅제약 중앙연구소)
  • Published : 1993.04.01
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Abstract

The synthesis and physicochemical properties of a novel cephalosporin, DWC-751 are described. DWC -751, (6R , 7R)-7-[ (Z)-2-(2-aminothiazol-4-yl)-2- methoxyiminoacetamido]-3-[(1-methylbenzotriazol-3-ium) methyl]-ceph-3-em-4-carboxylate monosulfate($IV_{\alpha}$) was conveniently obtained by the conversion of compound (IV) into the crystalline monosulfate. Adjusting pH 4.8-5.2 in aqeous solution of the crude crystalline, compound(IV) in the form of a crystalline pentahydrate was prepared with a high degree of purity. The influence of the various organic and inorganic acids on the solubility of compoud(IV) and its salts, was examined. Particularly, the solubility of DWC-751 was 92 mg/mι at pH 1.7 and 233 mg/mι at pH 3.0. DWC-751 showed a broad antimicrobial spectrum against gram-positive and negative bacteria.

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