摘要
三和四取代甲烷(TRSMs)是许多已批准的药物和前药物的重要结构基序。TRSM单元在药物化学中的应用越来越多,许多衍生物被专门设计用于通过围绕TRSM部分的新化学空间进行药物-靶相互作用。从这个角度来看,我们描述了获取一系列功能化选择性TRSMs及其分子作用机制的合成挑战,特别是作为抗感染的作用机制。与拥有更多sp2碳的平面基序相比,(+)-Bionectin A, B, (+)-Gliocladine C, Balanocarpol等天然抗感染蛋白具有选择性和有效的TRSMs与靶蛋白结合,这可能是由于构象减少了构象熵的惩罚,随着三维度的增强。本文还概述了阿米三嗪、艾芬地尔、巴瑞克替尼和瑞德西韦等再利用trsm的性质及其在COVID-19治疗中的最新进展和作用模式。这一观点有望为科学家、研究人员和学者提供用户指南和参考来源,以寻求新设计的TRSMs作为治疗方法。
关键词: 三和四取代甲烷,抗感染药、阿米三嗪、艾芬地尔、巴瑞克替尼和瑞德西韦
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