Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Huangpu Avenue 601, Guangzhou, China.
J Antibiot (Tokyo). 2011 Aug;64(8):571-81. doi: 10.1038/ja.2011.50. Epub 2011 Jul 20.
A set of 17 novel ketolides bearing an aryltetrazolyl-substituted alkyl side chain were synthesized and evaluated for their antibacterial activities, which the aryltetrazolyl group was selected to replace the hetero-aryl moiety of the side chain in telithromycin for designing new compounds. The synthesis of aryltetrazolyl alkylamines was reported in detail. The antibacterial activities of new ketolides were evaluated against a number of pathogens including macrolide-resistant organisms by using telithromycin as the reference. Many of the evaluated compounds exhibited remarkable activities against both erythromycin-susceptible and erythromycin-resistant organisms such as Staphylococcus aureus (except S. aureus AD-08), Pseudomonas aeruginosa and Escherichia coli. Among these, the compound 11e exhibited excellent antibacterial potency against all the strains in comparison with others.
一组 17 种新型酮内酯，带有一个芳基四唑基取代的烷基侧链，被合成并评估了其抗菌活性，其中芳基四唑基被选择取代泰利霉素侧链中的杂芳基部分，用于设计新化合物。详细报道了芳基四唑基烷基胺的合成。通过使用泰利霉素作为参比，评估了新酮内酯对包括耐大环内酯类药物的病原体在内的多种病原体的抗菌活性。许多评估的化合物对红霉素敏感和红霉素耐药的病原体如金黄色葡萄球菌（除 AD-08 金黄色葡萄球菌外）、铜绿假单胞菌和大肠杆菌均表现出显著的活性。其中，化合物 11e 与其他化合物相比，对所有菌株均表现出优异的抗菌效力。
