酰胺电子等排体在先导化合物优化中的应用

发布时间：2018-03-15 10:19

本文选题：酰胺　切入点：生物电子等排体　出处：《化学进展》2016年09期 　论文类型：期刊论文

【摘要】：生物电子等排体是指一类化合物或基团,这类物质拥有近似的分子形状和体积,类似的电子分布,并由此表现出相似的物理特性。作为激动剂或拮抗剂生物电子等排体能对相同的生化相关体系发挥作用,产生彼此互相相关的生物特性。药物结构中酰胺结构作为药效团和药物的重要组成部分被广泛应用。然而作为药物分子结构的重要组成部分,酰胺结构也存在着一些明显的缺点,包括代谢不稳定、代谢产物有毒和膜渗透性差等。为了克服这些缺点同时又想保持部分酰胺的特性,生物电子等排体替换是有效的方法之一。在先导化合物的优化过程中,通过酰胺生物电子等排体替换还能达到提高生物活性和靶点选择性、降低合成难度、扩展或突破知识产权限制等目的。本综述着重介绍了近五年来酰胺及其生物电子等排体在先导化合物优化过程中的应用。希望能对含有酰胺结构的先导化合物的优化提供新的思路,加速新药研发进程。
[Abstract]:A bioelectron equivalent is a class of compounds or groups that have similar molecular shapes and volumes, similar electron distributions, And it shows similar physical properties. As agonist or antagonist, bioelectron excretion plays an important role in the same biochemical related system. Producing interrelated biological properties. Amide structures are widely used as pharmacophore and important components of drugs in drug structures. However, as important components of drug molecular structures, The structure of amides also has some obvious disadvantages, including unstable metabolism, toxic metabolites and poor membrane permeability. In the process of optimization of leading compounds, amidebion isobaric substitution can improve biological activity and target selectivity, and reduce the difficulty of synthesis. This review focuses on the application of amides and their bioelectronic isobarkers in the optimization of lead compounds in the past five years. It is hoped that this review can be used for the optimization of lead compounds with amide-containing structures. Optimization provides new ideas, Speed up the development of new drugs.
【作者单位】：江苏食品药品职业技术学院药学院;
【分类号】：TQ460.1;O621.13

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