新活性红霉素衍生物的研究进展  

Recent developments in erythromycin derivatives with new bioactivities

作　　者：包凯[1] 张为革[1] 程卯生[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2009年第1期74-79,共6页Journal of Shenyang Pharmaceutical University

摘　　要：目的综述新活性红霉素衍生物的研究进展。方法依据国内外近期公开发表的30篇文献,对新活性红霉素衍生物的研究进展进行分类、归纳与总结。结果长期以来,红霉素及其衍生物作为抗菌药物被广泛使用。临床与实验数据显示,该类化合物还具有一些新的生物活性,例如促进消化道运动活性、抗炎与免疫调节活性、拮抗黄体生成素释放激素活性以及抑制磷酸二酯酶-3活性等。在提高红霉素的新活性并降低其抗菌作用的研究中,已设计、合成了多种类型的新结构的红霉素衍生物。结论利用红霉素衍生物的新活性研制、开发新药,已逐步成为红霉素衍生物研究的重要内容,呈现良好的发展势头。Objective To review the recent developments in erythromycin derivatives with new bioactivities. Methods According to the published papers and patents, the recent developments in erythromycin derivatives with new bioactivities were classified and summarized. Results Erythromycin and its derivatives had been widely used as antibacterial drugs for decades. Clinical and experimental data, however, indicated that they also have some new bioactivities, such as prokinetic effect, anti-inflammatory and immunomodulatory effect, luteinizing hormone-releasing hormone （LHRH） antagonistic effect and phosphodiesterase-3 inhibitory ac- tivity. In the effort to maximize these new activities of erythromycin while attenuate its anti-microbial effect, several series of novel erythromycin derivatives had been designed and synthesized. Conclusions The research and development of erythromycin derivatives with new bioactivities have gradually become an important part of erythromycin derivatives＇research,which possess a good prospect.

关 键 词：红霉素衍生物 生物活性 构效关系 

分 类 号：R914[医药卫生—药物化学]