Identification of Novel Benzoxa-[2,1,3]-diazole Substituted Amino Acid Hydrazides as Potential Anti-Tubercular Agents
作者:Alistair Brown、Ahmed Aljohani、Jason Gill、Patrick Steel、Jonathan Sellars
DOI:10.3390/molecules24040811
日期:——
medicines. Herein, we report the synthesis of a series of novel benzoxa-[2,1,3]-diazole substituted amino acid hydrazides in a two-step synthesis and evaluate their inhibitory activity against Mtb and selected bacterial strains of clinical importance utilising an end point-determined REMA assay. Alongside this, their potential for undesired cytotoxicity against mammalian cells was assessed employing standard
迫切需要发现和开发用于治疗结核分枝杆菌(Mtb)感染的新治疗方法,以解决该疾病持续的全球负担以及与现有药物相关的功效和成本限制。在这里,我们报告了两步合成中一系列新的苯并x- [2,1,3]-二唑取代的氨基酸酰肼的合成,并评估了它们对Mtb的抑制活性以及利用终点对某些具有临床意义的细菌的抑制作用测定的REMA测定。除此之外,使用标准MTT分析方法评估了它们对哺乳动物细胞产生不良细胞毒性的潜力。使用三个位点(肼,氨基酸,