Engineering Research Center of Environmental Materials and Membrane Technology of Hubei Province, School of Materials Science and Engineering, Wuhan Institute of Technology, Wuhan 430205, PR China.
Engineering Research Center of Environmental Materials and Membrane Technology of Hubei Province, School of Materials Science and Engineering, Wuhan Institute of Technology, Wuhan 430205, PR China.
Bioorg Chem. 2019 Oct;91:103133. doi: 10.1016/j.bioorg.2019.103133. Epub 2019 Jul 19.
The increase in antibiotic resistance due to various factors has encouraged the look for novel compounds which are active against multidrug-resistant pathogens. In this framework, chalcone-based compounds showed a diversity of pharmacological properties, and its derivatives possess a high degree of structural diversity, and it is helpful for the discovery of new therapeutic agents. The growing resistance to antibiotics worldwide has endangered their efficacy. This has led to a surging interest in the discovery of new antibacterial agents. Thus, there is an urgent need for new antibacterial drug candidates with increased strength, new targets, low cost, superior pharmacokinetic properties, and minimum side effects. The present review concluded and focuses on the recent developments in the area of medicinal chemistry to explore the diverse chemical structures of potent antibacterial agents and also describes its structure-activity relationships studies. The various synthetic structures leading to this class of neutral protective compound is common and additional structural optimization is promising for potential drug discovery and development.
由于各种因素导致抗生素耐药性的增加，促使人们寻找新型化合物来对抗多药耐药病原体。在这一框架内，查尔酮类化合物表现出多种药理特性，其衍生物具有高度的结构多样性，有助于发现新的治疗剂。全球范围内抗生素耐药性的增加危及到它们的疗效。这导致人们对发现新的抗菌剂产生了浓厚的兴趣。因此，迫切需要具有更强效力、新靶点、低成本、优越药代动力学特性和最小副作用的新型抗菌药物候选物。本综述总结并重点介绍了药物化学领域的最新发展，以探索具有强大抗菌活性的化合物的多样化化学结构，并描述了其构效关系研究。导致这类中性保护化合物的各种合成结构很常见，进一步的结构优化有望为潜在的药物发现和开发提供前景。
