Department of Life Science, School of Natural Sciences, Shiv Nadar University, Dadri, Uttar Pradesh, India.
Department of Chemistry, School of Natural Sciences, Shiv Nadar University, Dadri, Uttar Pradesh, India.
Drug Dev Res. 2019 Jun;80(4):490-503. doi: 10.1002/ddr.21523. Epub 2019 Feb 21.
Antimicrobial drug resistance is one of the most critical problems that plagued the human race in modern times. Discovery of novel antibiotics is important to counter this threat. Accordingly, herein we have reported the discovery of substituted benzimidazole class of molecules with antimicrobial property (specifically against Staphylococcus aureus). They were initially identified through a random screening and a novel catalytic synthetic strategy was utilized to access them. in vitro screening and phenotypic profiling revealed the antimicrobial nature. De novo transcriptome and gene analyses predicted the putative targets. This work provides a solid foundation for developing the benzimidazoles as a target specific antimicrobial preclinical candidate.
抗菌药物耐药性是困扰现代人类的最严重问题之一。发现新的抗生素对于应对这一威胁非常重要。因此，我们在此报告了具有抗菌特性（特别是针对金黄色葡萄球菌）的取代苯并咪唑类分子的发现。它们最初是通过随机筛选发现的，并利用一种新的催化合成策略来获得它们。体外筛选和表型分析揭示了它们的抗菌性质。从头转录组和基因分析预测了可能的靶标。这项工作为将苯并咪唑类药物开发为具有靶向性的抗菌临床前候选药物奠定了坚实的基础。
