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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Comparison of the efficiency of various methods for the synthesis of models of metabolites: example of 4a-methylhexahydronaphtalenones.
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Comparison of the efficiency of various methods for the synthesis of models of metabolites: example of 4a-methylhexahydronaphtalenones.

机译：各种代谢物模型合成方法的效率比较：4a-甲基六氢萘萘酮的实例。

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摘要

In order to examine the biotransformations of xenobiotics, it is essential to realize studies of metabolism of drugs in living animals. It is generally difficult to extract quantitatively the metabolites from biological media or excreta. Alternative methods have then been developed. Application of such techniques to 4a-methylhexahydronaphthalenones, which constitute starting material for the stereospecific synthesis of terpenoids or steroids, is particularly demonstrative. By biosynthetical ways, it was not possible to access with good yields to all the metabolites obtained in vivo. A novel methodology, based on the use of a manganoporphyrin catalyst, allowed to synthesize large amounts of several models of metabolites corresponding to those which had been isolated in living rats. Only one of the metabolites obtained in vivo could not be synthesized by this biomimetic system. This proved that alternative methods are precious to obtain models with good yields, but need to be validated by controls in living animals.
机译：为了检查异种生物的生物转化，实现对活体动物药物代谢的研究至关重要。通常很难从生物介质或排泄物中定量提取代谢产物。然后开发了替代方法。此类技术在构成4a-甲基六氢萘烯酮（构成萜类化合物或类固醇的立体定向合成的起始原料）中的应用特别具有示范性。通过生物合成方法，不可能以高产率获得体内获得的所有代谢产物。基于使用锰卟啉催化剂的新颖方法，可以合成大量与活体大鼠中分离出的代谢物相对应的几种模型。该仿生系统不能合成体内获得的一种代谢产物。这证明了替代方法对于获得具有良好产量的模型很有价值，但需要通过活体动物的对照进行验证。

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