Zhang Gui-Fu, Liu Xiaofeng, Zhang Shu, Pan Baofeng, Liu Ming-Liang
School of Nuclear Technology and Chemistry & Biology, Hubei University of Science and Technology, Hubei, PR China.
Zhejiang Xianju Junye Pharmaceutical Co., Ltd, Xianju, Zhejiang, 317300, PR China; School of Chemistry and Chemical Engineering, Wuhan University of Science and Technology, Wuhan, Hubei 430081, PR China.
Eur J Med Chem. 2018 Feb 25;146:599-612. doi: 10.1016/j.ejmech.2018.01.078. Epub 2018 Feb 4.
Bacterial infections represent a significant health threat globally, and are responsible for the majority of hospital-acquired infections, leading to extensive mortality and burden on global healthcare systems. The second generation fluoroquinolone ciprofloxacin which exhibits excellent antimicrobial activity and pharmacokinetic properties as well as few side effects is introduced into clinical practice for the treatment of various bacterial infections for around 3 decades. The emergency and widely spread of drug-resistant pathogens making ciprofloxacin more and more ineffective, so it's imperative to develop novel antibacterials. Numerous of ciprofloxacin derivatives have been synthesized for seeking for new antibacterials, and some of them exhibited promising potency. This review aims to summarize the recent advances made towards the discovery of ciprofloxacin derivatives as antibacterial agents and the structure-activity relationship of these derivatives was also discussed.
细菌感染在全球范围内对健康构成重大威胁，是大多数医院获得性感染的病因，导致大量死亡，并给全球医疗系统带来负担。第二代氟喹诺酮类药物环丙沙星具有出色的抗菌活性和药代动力学特性，且副作用较少，已应用于临床治疗各种细菌感染约30年。耐药病原体的出现和广泛传播使环丙沙星越来越无效，因此开发新型抗菌药物势在必行。为了寻找新的抗菌药物，人们合成了许多环丙沙星衍生物，其中一些显示出有前景的抗菌效力。本综述旨在总结环丙沙星衍生物作为抗菌剂的发现方面的最新进展，并讨论这些衍生物的构效关系。
