Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Odbojarov 10, 83232 Bratislava, Slovakia.
Curr Med Chem. 2018;25(38):4972-5006. doi: 10.2174/0929867324666170918122633.
Emerging resistance of bacterial pathogens to clinically used drugs, including not only first-choice but also second- and third-choice drugs, is alarming, but since the 1990s only a modest number of new, first in class, drugs for systemic administration have been marketed for the treatment of bacterial infections.
This article provides a review of recently reported new antibacterial chemotherapeutics approved for clinical practice, antibacterial chemotherapeutics in clinical trials and antibacterial agents under development.
Antibacterial agents include new antibacterial compounds of used drug classes and new antibacterial agents with a novel mode of action. In addition, particular attention is given to agents decreasing bacterial resistance, i.e. to compounds that do not have significant intrinsic bacteriostatic or bactericidal activity, but in combination with antibacterial drugs are able to restore the effect of these drugs or demonstrate synergistic antibacterial properties together with the drugs.
This review is specifically focused on small molecules rather than on peptides and discusses a wide range of various molecular scaffolds.
包括一线、二线甚至三线药物在内，临床应用的抗菌药物的耐药性不断增强，令人担忧。但自 20 世纪 90 年代以来，仅有少数新型、作用机制独特的全身性抗菌药物上市，用于治疗细菌感染。
本文对近期获准临床应用的新型抗菌化学疗法、临床试验中的抗菌化学疗法以及正在研发中的抗菌药物进行了综述。
抗菌药物包括新型抗菌化合物和作用机制独特的新型抗菌药物。此外，特别关注降低细菌耐药性的药物，即那些没有显著固有抑菌或杀菌活性的化合物，但与抗菌药物联合使用时，能够恢复这些药物的疗效，或者与药物联合具有协同抗菌作用。
本综述主要关注小分子，而非肽类，并讨论了各种不同的分子骨架。
