Zhang Zhongjing College of Traditional Chinese Medicine, Nanyang Institute of Technology, Nanyang, 473004, Henan, China.
Henan Key Laboratory of Zhang Zhongjing Formulae and Herbs for Immunoregulation, Nanyang, 473004, Henan, China.
Curr Top Med Chem. 2022;22(12):1020-1034. doi: 10.2174/1568026622666220317162132.
Staphylococcus aureus (S. aureus), an important pathogen of both humans and animals, can cause a variety of infections at any site of the body. The evolution of S. aureus resistance is notorious, and the widespread of drug-resistant S. aureus, especially methicillin-resistant S. aureus (MRSA), has made the treatment difficult in recent decades. Nowadays, S. aureus is among the leading causes of bacterial infections, creating an urgent need for the development of novel antibacterial agents. Ciprofloxacin, characterized by high clinical efficacy, is a broad-spectrum antibacterial agent with frequency of prescription for various Gram-positive and Gram-negative pathogens, many of which are resistant to a wide range of antibiotics. However, the long-term and widespread use of this antibiotic has led to the emergence of ciprofloxacin-resistant pathogens, and ciprofloxacin- resistant S. aureus has been noted in clinical practice. Ciprofloxacin hybrids have been recognized as advanced chemical entities to simultaneously modulate multiple drug targets in bacteria, so ciprofloxacin hybrids have the potential to overcome drug resistance. The present review provides an overview of ciprofloxacin hybrids with anti-S. aureus potential that has been reported in the last decade with an emphasis on their structure-activity relationships and mechanisms of action.
金黄色葡萄球菌（S. aureus）是人和动物的重要病原体，可在身体的任何部位引起多种感染。S. aureus 的耐药性演变是臭名昭著的，近年来耐药性金黄色葡萄球菌（MRSA）的广泛传播使得治疗变得困难。如今，S. aureus 是细菌性感染的主要原因之一，迫切需要开发新型抗菌药物。环丙沙星具有临床疗效高的特点，是一种广谱抗菌药物，常用于治疗多种革兰氏阳性和革兰氏阴性病原体，其中许多病原体对多种抗生素具有耐药性。然而，这种抗生素的长期和广泛使用导致了对环丙沙星耐药的病原体的出现，并且在临床实践中已经注意到了对环丙沙星耐药的金黄色葡萄球菌。环丙沙星杂合药物已被认为是一种先进的化学实体，可以同时调节细菌中的多个药物靶点，因此环丙沙星杂合药物有可能克服耐药性。本综述介绍了过去十年中报道的具有抗金黄色葡萄球菌潜力的环丙沙星杂合药物，重点介绍了它们的结构-活性关系和作用机制。
