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新型氟喹诺酮衍生物与碳水化合物偶联物的合成及抗结核活性评价。

Synthesis and antitubercular evaluation of new fluoroquinolone derivatives coupled with carbohydrates.

机构信息

Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, Brazil.

出版信息

Carbohydr Res. 2010 Apr 19;345(6):761-7. doi: 10.1016/j.carres.2010.01.016. Epub 2010 Feb 1.

Abstract

We describe in this work the synthesis of nine new fluoroquinolone derivatives based on modifications at the C-7 position of the known fluoroquinolones cipro-, gati-, and moxifloxacin, as well as their antitubercular evaluation. The synthesis of these new analogues was improved using microwave irradiation, providing several advantages such as better yields and shorter reaction times, in comparison with classical reaction conditions. Derivatives 4, 5, and 7 exhibited promising antitubercular activities.

摘要

在这项工作中,我们描述了基于已知氟喹诺酮环丙沙星、加替沙星和莫西沙星 C-7 位修饰的九种新型氟喹诺酮衍生物的合成及其抗结核活性评价。与经典反应条件相比,微波辐射的使用改进了这些新类似物的合成,提供了更好的产率和更短的反应时间等优势。衍生物 4、5 和 7 表现出有前景的抗结核活性。

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