Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, PR China.
J Antibiot (Tokyo). 2012 Feb 15. doi: 10.1038/ja.2012.3.
Novel azithromycin (AZM) derivatives with the C-4″ bisamide side chains were synthesized and evaluated for their in vitro antibacterial activities. The 4″-O-(benzamido)alkyl carbamates showed excellent activity against the erythromycin-susceptible Streptococcus pneumoniae and exhibited greatly improved activity against erythromycin-resistant S. pneumoniae. Among them, compounds 5g and 6g, which had the same electron-withdrawing group, 3,5-dinitrophenyl, on the termination of their C-4″ bisamide side chains, demonstrated the most potent activity against erythromycin-resistant S. pneumoniae expressing the erm gene, the mef gene and the erm and mef genes, showing 128-fold, 33-fold and 32-fold improved activity in comparison with the parent AZM.The Journal of Antibiotics advance online publication, 15 February 2012; doi:10.1038/ja.2012.3.
新型阿奇霉素（AZM）衍生物的 C-4″双酰胺侧链被合成，并评估其体外抗菌活性。4″-O-（苯甲酰胺）烷基氨基甲酸酯对红霉素敏感的肺炎链球菌表现出极好的活性，并且对红霉素耐药的肺炎链球菌表现出大大改善的活性。其中，化合物 5g 和 6g 在 C-4″双酰胺侧链的末端具有相同的吸电子基团 3,5-二硝基苯基，对表达 erm 基因、mef 基因和 erm 和 mef 基因的红霉素耐药肺炎链球菌表现出最强的活性，与亲本 AZM 相比，其活性提高了 128 倍、33 倍和 32 倍。《抗生素杂志》在线提前出版，2012 年 2 月 15 日；doi:10.1038/ja.2012.3.
