瑞德西韦的合成、作用机制与应用

Synthesis,Mechanism and Application of Remdesivir

瑞德西韦是一种具有广谱抗RNA病毒活性的核苷类似物,通过抑制病毒中RNA依赖性的RNA聚合酶活性从而发挥作用。在药物设计中,首先筛选了具有抑制病毒生长活性的核苷类似物,确定了鸟嘌呤类似物和戊糖的基本结构,再对其进行磷酸修饰、前药修饰和实验筛选得到最终结构。在药物合成方面,通过对两代合成路线的对比,讨论了反应条件和手性合成对其合成效率的影响,强调反应条件和立体化学在合成中的重要作用。在应用方面,概要阐述了在各类RNA病毒病治疗中的实验和应用情况。通过上述介绍,以期对瑞德西韦有一个相对全面的认识。

Remdesivir is a nucleoside analogue with broad spectrum anti-RNA virus activity,which acts by in hibiting RNA-dependent RNA polymerase activity of the virus.The drug synthesis had three steps of screening nu cleoside analogues which can inhibit the growth activity of virus,determining the basic structure of guanine ana logues and pentose and conducting phosphoric acid modification,prodrug modification and experimental screening to obtain its structure.The effects of reaction conditions and chiral synthesis on the synthesis efficiency are dis cussed by comparing the two generation synthesis routes.Finally,the experimental and application of remdesivir in the treatment of various RNA viruses are discussed in order to have a comprehensive understanding of remdesivir.