摘要
通过分析发色团、硫交联桥、核心环缩肽及其氨基酸组成与其抗菌活性的关系,对一组喹喔啉类抗生素进行了定性构效关系研究。结果显示,发色团对活性有一定影响,具喹喔啉发色团的化合物抗菌活性高于喹啉发色团,6位溴取代喹啉发色团可能有利于抗菌活性的提高;硫缩醛交联桥对活性的贡献优于甲基化的二硫桥,交联桥的烷基化程度对活性也有影响,核心环缩肽的存在是维持抗菌活性的必要条件。
Structure-activity relationship（SAR） analysis of quinoxaline antibiotics was discussed. The resuits showed that chromophores played a major role in efforts on the biological activity, and the compounds with quinoxaline chromophores had higher aitivities than those w.ith quinoline chromophores. Meanwhile, the 6-bromo substituted quionoline chromophores might be benefit to improve the antimicrobial activity. The existence of sulfur containing cross-linkage was essential to keep high antimicrobial activity and thioacetal cross-bridge made greater contribution than disulphide cross-linkage to antimicrobial activity. It was necessary for the central core depsipeptide to maintain antimicrobial activity and its components of amino acid had some effects on antimicrobial activity.
出处
《化学与生物工程》
CAS
2008年第6期1-4,共4页
Chemistry & Bioengineering
基金
国家自然科学基金资助项目(30271486)
国家863项目(2006AA10A29)
关键词
喹喔啉类抗生素
构效关系
抗菌活性
研究进展
quinoxaline antibiotics
structure-activity relationship （SAR）
antimicrobial activity
reasearch progress
