School of Chemistry, University of Leeds, Leeds LS2 9JT, UK.
School of Chemistry, University of Leeds, Leeds LS2 9JT, UK.
Bioorg Chem. 2014 Aug;55:69-76. doi: 10.1016/j.bioorg.2014.05.008. Epub 2014 Jun 2.
In recent years bacterial resistance has been observed against many of our current antibiotics, for instance most worryingly against the cephalosporins which are typically the last line of defence against many bacterial infections. Additionally the failure of high throughput screening in the discovery of new antibacterial drug leads has led to a decline in the number of antibacterial agents reaching the market. Alternative methods of drug discovery including structure based drug design are needed to meet the threats caused by the emergence of resistance. In this review we explore the latest advancements in the identification of new antibacterial agents through the use of a number of structure based drug design programs.
近年来,我们现有的许多抗生素都出现了细菌耐药性,最令人担忧的是,头孢菌素类抗生素通常是治疗许多细菌感染的最后一道防线。此外,高通量筛选在发现新的抗菌药物先导化合物方面的失败,导致进入市场的抗菌药物数量减少。需要包括基于结构的药物设计在内的替代药物发现方法来应对耐药性出现带来的威胁。在这篇综述中,我们探讨了通过使用多种基于结构的药物设计程序来鉴定新的抗菌药物方面的最新进展。