本文選題：FXa + 藥物化學(xué)　； 參考：《藥學(xué)學(xué)報》2015年10期

【摘要】：新藥創(chuàng)制是復(fù)雜的智力活動,涉及科學(xué)研究、技術(shù)創(chuàng)造、產(chǎn)品開發(fā)和醫(yī)療效果等多維科技活動。每個藥物都有自身的研發(fā)軌跡,而構(gòu)建化學(xué)結(jié)構(gòu)是最重要的環(huán)節(jié),因為它涵蓋了藥效、藥代、安全性和生物藥劑學(xué)等性質(zhì)。本欄目以藥物化學(xué)視角,對有代表性的藥物的成功構(gòu)建,加以剖析和解讀。利伐沙班是首創(chuàng)的預(yù)防血栓形成的FXa抑制劑,基于藥物化學(xué)的理念和方法,通過合成-活性評價的試錯操作(trail and error),優(yōu)化了藥效學(xué)和藥動學(xué),最終獲得了上市的利伐沙班,經(jīng)結(jié)構(gòu)生物學(xué)證實該分子結(jié)構(gòu)演繹的合理性,與基于受體結(jié)構(gòu)的分子設(shè)計有異曲同工之妙。
[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.
【作者單位】： 中國醫(yī)學(xué)科學(xué)院藥物研究所;
【分類號】：R973

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