摘要
设计合成了１０个７βＮ２芳基三嗪酰胺基苯乙酰胺基３亚甲基杂环头孢烯酸衍生物及其二钠盐，均为未见文献报道的新化合物，其结构经元素分析数据及光谱分析证实．体外抑菌试验结果表明：化合物（Ⅱ１），（Ⅱ２）和（Ⅱ３）活性较强，对所选用的１９种菌株均有一定的活性，多数化合物的ＭＩＣ值为８ｍｇ／Ｌ。
We are to report the design,synthesis and evaluation of the ten derivatives of 7β 2 ( N 2 aryl triazinoylamido) 2 phenylacetamido 3 methylene heterocyclic cephalosporins in the paper.They were prepared by the acylation of corresponding pentachlorophenol ester of 2 aryl 1,2,4 triazine 3,5 dione 6 carboxylic acid with 7 ( D α aminophenyl acetamido) 3 methylene heterocyclic cephalosporin at room temperature.All of these target compounds are new compounds,whose structures were characterized by elemental analysis,IR and 1H NMR spectra.The chemical entities were tested against S.aureus, E.coli,K.aerogenes and P.aeruginosa including MRSA 292 and three of them have significant antibacterial activities.The implication of these results on the SAR of antibacterial activity in this class will be discussed.
出处
《中国药物化学杂志》
CAS
CSCD
1999年第1期1-6,共6页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金资助
关键词
杂环头孢烯酸
三嗪青霉素
抗菌活性
合成
β
2 ( N 2 aryl triazinoylamido) 2 phenylacetamido
3 methylene heterocyclic cephalosporins
BL P 1908
antibacterial activity
