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

Synthesis of New Medicinal Agents (Ⅱ) : Synthesis and Antibacterial Activities of New Cephalosporin Derivatives

새로운 cephalosporin 항생물질인 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-heterocyclothiomethyl-3-cephem-4-carboxylic acid 유도체(2a∼2d)들을 합성하여, 구조변화에 대한 항균활성을 측정하였다. 그 중에서 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-[(2-methyl-1,3,4-thiadiazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid가 그람양성 및 음성균에 대하여 광범위한 향균능력ㅇ르 나타내었다.

New cephalosporin antibiotics, 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-heterocyclothiomethyl-3-cephem-4-carboxylic acid derivatives(2a∼2d) were synthesized. Antibacterial activities of these new cephalosporin derivatives and the relationship between their structures and their activities were examined. Among them,7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-[(2-methyl-1,3,4-thiadiazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid exhibited the broad antibacterial activities against Gram(+) and Gram(-) bacteria.