摘要
背景:唑类化合物因其活性范围广、疗效高、耐受性好、可口服等特点,已成为制药行业中广泛应用的支架药物。此外,唑类衍生物作为有效的抗菌药物已引起人们的关注。 导论:本文综述了2016-2020年报道的具有抗菌活性的主要唑类支架药物的药理方面,包括咪唑、苯并咪唑、三唑和四唑,以及我们在该领域的所有出版物。此外,我们还讨论了唑类衍生物的结构与活性的关系以及分子对接研究,为合成具有良好生物活性的新型唑类化合物提供了重要特征和有价值的信息。本综述中提出的结构已经对几种细菌和真菌进行了测试,如大肠杆菌和白色念珠菌,这些细菌和真菌在所有这些研究中都很常见。 结果:对所测化合物的MIC进行比较,发现氟康唑基结构的抗真菌活性最强,而三唑类含硝基苯和香豆素基团的衍生物抑菌活性最强。 结论:与苯并咪唑、四唑等其他唑类衍生物相比,三唑、咪唑类支架对抗菌化合物的设计更为重要。所有活性最高的化合物都符合利平斯基规则。
关键词: 唑,抗菌,分子对接,SAR, MIC, Lipinski规则
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