氧化:前药物生物前体活化的最常见途径

S. Saied, Mohanad Saleh, Salim Mohammed
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引用次数: 0

摘要

无活性前药的氧化(它们的作用方式不是通过链接载体,而是通过修饰它们的分子,称为生物前体)到活性母药设计通常是通过方法修饰策略,旨在改善药物的物理化学和药理学特性,如增加生物利用度,水溶性和/或作用持续时间。这些前药需要代谢或化学转化反应才能转变为它们的活性药物,这些化学反应一般是通过质子活化、消除活化、氧化活化、还原活化和磷酸化活化或脱羧活化等I相反应形成的。本文综述了前体药物氧化活化的最新进展,如n -和o-氧化脱烷基、氧化脱胺、n -氧化和s -氧化等重要策略在制备亲本活性药物中的应用。氧化反应是非常重要的,大多数癌症都是从这些反应开始的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Oxidation: The Most Common Pathway for the Pro-drugs Bio Precursors Activation
Oxidation of inactive prodrug (that their mode of action is not via linkage carrier, but occur through modification of their molecules which are called the bio precursor) to active parent drug design is generally via the methods modification strategies that aim to improve the physicochemical and pharmacological properties of drugs such as increases bioavailability, water solubility and/or duration of action. These prodrugs need metabolically or chemical transformation reactions to change to their active drugs, these chemical reactions are generally formed by phase I reactions through proton activation, elimination activation, oxidative activation, reductive activation and phosphorylation activation or decarboxylation activation. The goal of this review is to study the up-to-date advances in the prodrug’s oxidative activation such as N-and O-oxidative dealkylation, oxidative deamination, N-oxidative and S-oxidative important strategies to produce the parents’ active drugs. Oxidation reactions are of great importance and most cancerous diseases begin with these reactions.
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