A novel series of 3-O-arylalkylcarbamoyl-3-O-descladinosyl-9-O-(2-chlorobenzyl)oxime clarithromycin derivatives, were designed, synthesized and evaluated for their in vitro antibacterial activity. These derivatives were found to have strong activity against susceptible and resistant bacteria strains. Among them, compounds 7a and 7q showed the most potent activity (0.125 µg/mL) against erythromycin-resistant S. pneumoniae expressing the mefA gene. Moreover, compounds 7f, 7i, 7p and 7z displayed remarkably improved activity (4 µg/mL) against penicillin-resistant S. aureus ATCC31007, and compounds 7a, 7b, 7f, 7p and 7z showed improved activity (8 µg/mL) against erythromycin-resistant S. pyogenes. In particular, compound 7z exhibited potent and balanced activity against the tested drug-susceptible and -resistant bacterial strains.

一种新型系列3- ö -arylalkylcarbamoyl -3- ö -descladinosyl -9- ø -克拉霉素衍生物（2-氯苄基）肟，设计，合成并评价了它们的体外抗菌活性。发现这些衍生物对易感和抗性细菌菌株具有很强的活性。其中，化合物7a和7q对表达mef A基因的耐红霉素的肺炎链球菌具有最强的活性（0.125 µg / mL）。此外，化合物7f，7i，7p和7z的抗青霉素活性显着提高（4 µg / mL）金黄色葡萄球菌ATCC31007以及化合物7a，7b，7f，7p和7z对耐红霉素的化脓性链球菌显示了更高的活性（8 µg / mL）。特别地，化合物7z对测试的药物敏感性和抗性细菌菌株表现出有效和平衡的活性。