Emami Saeed, Shafiee Abbas, Foroumadi Alireza
Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
Mini Rev Med Chem. 2006 Apr;6(4):375-86. doi: 10.2174/138955706776361493.
A major recent focus of quinolone antibacterials has been the development of agents with enhanced activity against Gram-positive bacteria. The extensive research efforts have enabled a better definition of the structural features of quinolones that offer the best combination of clinical efficacy and reduced resistance selection in Gram-positive bacteria. This review considers the structural features of new quinolones and relationship to antibacterial activity against Gram-positive bacteria, while trying to position them in the context of recent and possible future advances based on an understanding of their chemical structure and how these impact on target specificity, avoidance of efflux and prevention of emergence of quinolone-resistant mutants in Gram-positive bacteria.
喹诺酮类抗菌药物近期的一个主要关注点是开发对革兰氏阳性菌活性增强的药物。广泛的研究工作使得能够更好地界定喹诺酮类药物的结构特征，这些特征在革兰氏阳性菌中提供了临床疗效和降低耐药性选择的最佳组合。本综述考虑了新型喹诺酮类药物的结构特征及其与对革兰氏阳性菌抗菌活性的关系，同时基于对其化学结构的理解以及这些结构如何影响靶点特异性、避免外排和防止革兰氏阳性菌中喹诺酮耐药突变体的出现，试图将它们置于近期和未来可能进展的背景下。
