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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Design, synthesis and antibacterial activity of novel ketolides bearing an aryltetrazolyl-substituted alkyl side chain.
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Design, synthesis and antibacterial activity of novel ketolides bearing an aryltetrazolyl-substituted alkyl side chain.

机译：带有芳基四唑基取代的烷基侧链的新型酮醇化物的设计，合成和抗菌活性。

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摘要

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.
机译：合成了一组17个带有芳基四唑基取代的烷基侧链的新颖酮醇化物，并评估了它们的抗菌活性，选择了芳基四唑基团来代替替利霉素的侧链的杂芳基部分，以设计新化合物。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考，评估了新型酮酚对许多病原体（包括对大环内酯类耐药的生物）的抗菌活性。许多被评估的化合物对易感红霉素和抗红霉素的生物均显示出显着活性，例如金黄色葡萄球菌（金黄色葡萄球菌AD-08除外），铜绿假单胞菌和大肠杆菌。其中，化合物11e与所有菌株相比对所有菌株均显示出优异的抗菌效力。

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