摘要
背景:细菌性病原体对临床使用的药物(包括首选药物和第二和第三选择药物)产生的耐药性令人担忧,但自20世纪90年代以来,用于治疗细菌感染的系统性给药的新的、一流的药物数量很少。 前言:本文回顾了最近报道的临床实践批准的新型抗菌化疗药物,临床试验中的抗菌化疗药物和正在开发的抗菌药物。 讨论:抗菌剂包括已用药物类别的新抗菌化合物和具有新作用方式的新抗菌剂。此外,还特别注意降低细菌耐药性的药剂,即不具有显著的内在抑菌或杀菌活性的化合物,但与抗菌药物结合能够恢复这些药物的效果或与这些药物一起表现出协同抗菌性能。 结论:本综述的重点是小分子,而不是多肽,并讨论了各种各样的分子支架。
关键词: 抗菌化疗,临床试验,设计开发,外排泵抑制剂,耐药性,小分子,协同作用。
Current Medicinal Chemistry
Title:Design and Discovery of New Antibacterial Agents: Advances, Perspectives, Challenges
Volume: 25 Issue: 38
关键词: 抗菌化疗,临床试验,设计开发,外排泵抑制剂,耐药性,小分子,协同作用。
摘要: Background: 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.
Objective: 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.
Discussion: 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.
Conclusion: This review is specifically focused on small molecules rather than on peptides and discusses a wide range of various molecular scaffolds.
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Design and Discovery of New Antibacterial Agents: Advances, Perspectives, Challenges, Current Medicinal Chemistry 2018; 25 (38) . https://dx.doi.org/10.2174/0929867324666170918122633
DOI https://dx.doi.org/10.2174/0929867324666170918122633 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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