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Journal of the Korean Chemical Society (JKCS)

ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 36, Number 2
JKCSEZ 36(2)
April 20, 1992 

 
Title
Studies on the Synthesis and Antibacterial Activity of New β-Lactam Antibiotics

새로운 베타락탐 항생물질의 합성과 생물활성에 관한 연구
Author
Tae Heung Song, Young Ho Kim

송태흥, 김영호
Keywords
Abstract
신규 cephalosporin계 항생제로서, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-oxyiminoacetamido]-3-(4,6-diamino-1-alkyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylate의 유도체들을 합성하였다. 7-위치의 side chain에 있는 oxyimino 부위를 변화시켜서, 구조 변화에 따른 항균 활성의 변화를 측정하였다. 그 결과, 3-위치에서 4,6-diamino-1-methyl-1,3,5-triazinium-2-yl group을 가지며, 또한 7-α-methoxyimino기를 가진, C-1유도체가 가장 강력하고도 광범위한 항균활성을 그람 양성과 그람 음성 bacteria에 대하여 나타내었다.

The synthesis of a series of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-oxyiminoacetamido]-3-(4,6-diamino-1-alkyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylates is described. Variations of an oxyimino moiety in the 7-side chain and quaternary ammonium moiety in the 3-side chain were examined and structure-activity relationship was studied. The 4,6-diamino-1-methyl-1,3,5-triazinium-2-yl derivative of the 7-α-methoxyimino series of cephalospoins, particularly 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido]-3-(4,6-diamino-1-methyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylate(C-1), exhibited broad antibacterial activity against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa.

Page
293 - 300
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