School of Chemistry and Chemical Engineering, Yulin University, Yulin, 719000, Shaanxi, PR China; Shaanxi Key Laboratory of Low Metamorphic Coal Clean Utilization, Yulin University, Yulin, 719000, Shaanxi, PR China.
School of Chemistry and Chemical Engineering, Yulin University, Yulin, 719000, Shaanxi, PR China; Shaanxi Key Laboratory of Low Metamorphic Coal Clean Utilization, Yulin University, Yulin, 719000, Shaanxi, PR China.
Eur J Med Chem. 2021 Jan 1;209:112886. doi: 10.1016/j.ejmech.2020.112886. Epub 2020 Sep 29.
With the increasing number of cases of inactive and drug-resistance tuberculosis, there is an urgent need to develop new potent molecules set for fighting this brutal disease. Medicinal chemistry concerns the discovery, the development, the identification, and the interpretation of the mode of action of biologically active compounds at the molecular level. Molecules bearing oxadiazoles are one such class that could be considered to satisfy this need. Oxadiazole regioisomers have been investigated in drug discovery programs for their capacity to go about as powerful linkers and as pharmacophoric highlights. Oxadiazoles can go about as bioisosteric substitutions for the hydrazide moiety which can be found in first-line anti-TB drugs, and some have been likewise answered to cooperate with more current anti-TB targets. This present review summarizes the current innovations of oxadiazole-based derivatives with potential antituberculosis activity and bacteria discussing various aspects of structure-activity relationship (SAR).
随着非活动性和耐药性结核病病例的不断增加，迫切需要开发新的有效分子来对抗这种严重疾病。药物化学涉及在分子水平上发现、开发、鉴定和解释生物活性化合物的作用模式。含有恶二唑的分子就是这样一类可以满足这一需求的分子。恶二唑的区域异构体已经在药物发现计划中进行了研究，因为它们具有作为强大连接子和药效团突出物的能力。恶二唑可以作为在一线抗结核药物中发现的酰肼部分的生物等排体替代物，有些也被发现与当前的抗结核靶点协同作用。这篇综述总结了具有潜在抗结核活性和细菌作用的基于恶二唑的衍生物的最新创新，讨论了结构-活性关系（SAR）的各个方面。
