氟化前列环素的合成及生物学研究。

W. E. Barnette
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引用次数: 27

摘要

氟化已广泛用于类固醇领域,利用氢和氟的大小相似及其强电负性来改变和(或)增强活性并增加化学或生物稳定性。因此,发现同样的原理也适用于前列腺素,更具体地说是前列腺环素,这并不奇怪。前列环素的比活性和高不稳定性使其成为类似氟化技术的理想候选物。本文将讨论氟化类似物的设计和制备,以提高这一重要分子的化学和代谢稳定性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The synthesis and biology of fluorinated prostacyclins.
Fluorination has been used extensively in the steroid field to alter and/or enhance activity and to increase chemical or biological stability taking advantage of the similarity in size between hydrogen and fluorine and its strong electronegativity. Thus, it is not surprising to find that the same principle has been applied to prostaglandins, more specifically prostacyclin. The specific activity and high instability of Prostacyclin make it an ideal candidate for similar fluorination techniques. The design and preparation of fluorinated analogs with the aim of improving the chemical and metabolic stability of this important molecule will be discussed.
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