首创的FXa抑制剂利伐沙班

发布时间：2018-04-10 13:52

本文选题：FXa + 药物化学　；参考：《药学学报》2015年10期

【摘要】：新药创制是复杂的智力活动,涉及科学研究、技术创造、产品开发和医疗效果等多维科技活动。每个药物都有自身的研发轨迹,而构建化学结构是最重要的环节,因为它涵盖了药效、药代、安全性和生物药剂学等性质。本栏目以药物化学视角,对有代表性的药物的成功构建,加以剖析和解读。利伐沙班是首创的预防血栓形成的FXa抑制剂,基于药物化学的理念和方法,通过合成-活性评价的试错操作(trail and error),优化了药效学和药动学,最终获得了上市的利伐沙班,经结构生物学证实该分子结构演绎的合理性,与基于受体结构的分子设计有异曲同工之妙。
[Abstract]:New drug creation is a complex intellectual activity involving multi-dimensional scientific and technological activities such as scientific research, technological creation, product development and medical effects.Each drug has its own R & D track, and the construction of chemical structures is the most important step because it covers pharmacodynamics, pharmacology, safety and biopharmaceutical properties.This column analyzes and interprets the successful construction of representative drugs from the perspective of drug chemistry.Lipashaban is the first FXa inhibitor to prevent thrombosis. Based on the idea and method of pharmacochemistry, pharmacodynamics and pharmacokinetics were optimized by trail and errorosine, which was used to evaluate synthesis-activity, and finally the listed rivastaban was obtained.It is proved by structural biology that the deductive rationality of the molecular structure is similar to that of the molecular design based on the receptor structure.
【作者单位】：中国医学科学院药物研究所;
【分类号】：R973

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