The strategic use of fluorine substitution in drug discovery and drug development is well documented. The small size and high electronegativity of fluorine are among properties of this element that lend special advantages. Applications in drugs targeted to the central nervous system (CNS) have been particularly fruitful in addition to favorable properties seen in many peripherally acting drugs. Fluorine substitution can be used to solve problems unique to the CNS, such as blood brain barrier (BBB) penetration. Likewise, use of the positron emitting isotope, (18)F, provides a unique tool for non-invasive imaging and diagnoses in the CNS. In this review, fluorine in CNS drugs and drug discovery are discussed.

译文

:氟取代在药物发现和药物开发中的战略用途已得到充分证明。氟的小尺寸和高电负性是该元素的特性之一,具有特殊的优势。除了在许多外围作用药物中看到的有利特性外,在针对中枢神经系统(CNS)的药物中的应用也特别富有成果。氟取代可用于解决CNS独有的问题,例如血脑屏障(BBB)渗透。同样,正电子发射同位素(18)F的使用为CNS中的非侵入性成像和诊断提供了独特的工具。在这篇综述中,讨论了中枢神经系统药物中的氟和药物发现。

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