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氟化前列环素的合成与生物学

The synthesis and biology of fluorinated prostacyclins.

作者信息

Barnette W E

出版信息

CRC Crit Rev Biochem. 1984;15(3):201-35.

PMID:6370595
Abstract

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.

摘要

氟化作用已在甾体领域中广泛应用,利用氢和氟在大小上的相似性及其强电负性来改变和/或增强活性,并提高化学或生物稳定性。因此,发现相同的原理已应用于前列腺素,更具体地说是前列环素,也就不足为奇了。前列环素的特定活性和高不稳定性使其成为类似氟化技术的理想候选物。本文将讨论旨在提高这一重要分子的化学和代谢稳定性的氟化类似物的设计与制备。

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