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General Review Article

三唑并嘧啶核：用于开发具有适当药代动力学特征的抗病毒药物的特权支架

卷 29, 期 8, 2022

发表于: 23 August, 2021

页: [1379 - 1407] 页: 29

弟呕挨: 10.2174/0929867328666210526120534

价格: $65

摘要

病毒是对全球健康的持续威胁。针对某些病毒感染的治疗设备缺乏或有限以及耐药性问题的增加使得寻找新的抗病毒药物变得紧迫。近年来，越来越多的文献强调了三唑并嘧啶 (TZP) 杂环化合物在抗病毒药物开发中的应用，其中许多化合物对不同的 RNA 和 DNA 病毒显示出有效的抗病毒活性。 TZP 核心代表了获得生物活性分子的特权支架，这要归功于：i）允许在细胞核的不同位置对 TZP 进行各种功能化的合成可行性，ii）TZP 核心与分子靶点建立多重相互作用的能力， iii) 其有利的药代动力学特性。在本综述中，在提及具有不同生物活性的基于 TZP 的化合物的选定示例后，我们将重点关注过去 10 年文献中出现的那些抗病毒药物。将描述用于识别它们的方法、hit-to-lead 研究和出现的结构-活性关系。还将提及制备 TZP 核的合成方法。此外，还将分析它们的作用机制、生物靶标内的结合模式和药代动力学特性，突出基于 TZP 支架的化合物的优缺点，该支架越来越多地用于药物化学。

关键词: 三唑并嘧啶、病毒、小分子、抗病毒药物、药代动力学特性、药物化学、病毒聚合酶

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