摘要
目的设计合成2′,4″-二乙酰基红霉素-9-O-杂环烷基肟衍生物,并对其体内抗菌活性进行评价。方法以红霉素为原料,经9位羰基肟化、肟羟基烷基化、2′,4″-二羟基乙酰化3步反应制得目标化合物;选取有代表性的8个化合物评价其对小鼠感染所致败血症的治疗作用。结果与结论共制得18个未见文献报道的目标化合物,经MS1、H-NMR确证结构;该类化合物具有较好的抗菌活性,其中化合物9n的活性优于对照药罗红霉素和克拉霉素。
Aim To synthesize 2＇, 4＂-diacetyl-O-alkylerythromycin-9-oxime ether derivatives and to evaluate their antibacterial activities in vivo. Methods Starting from erythromycin, the target compounds were synthesized by the way of oximation, alkylation, acylation. Eight representative compounds were selected to evaluate their an- tibacterial activities in vivo. Results and conclusion Eighteen new compounds were prepared and their structures were determined by MS and ^1H-NMR. Some of these compounds had moderate antibacterial activities. Among them, 9n had better antibacterial activity than each of roxithromycin and clarithromycin.
出处
《中国药物化学杂志》
CAS
CSCD
2007年第2期72-77,共6页
Chinese Journal of Medicinal Chemistry
关键词
红霉素衍生物
抗菌活性
罗红霉素
克拉霉素
erythromycin derivatives
antibacterial activity
roxithromycin
clarithromycin
