Koufaki Maria, Detsi Anastasia
National Hellenic Research Foundation, Institute of Organic and Pharmaceutical Chemistry, Athens, Greece.
Methods Mol Biol. 2010;594:297-309. doi: 10.1007/978-1-60761-411-1_21.
The design and synthesis of hybrid molecules encompassing two pharmacophores in one molecular scaffold is a well-established approach to the synthesis of more potent drugs with dual activity. In this chapter, we will present the most important synthetic methodologies we have applied for the preparation of hybrid compounds containing the "universal antioxidant" alpha-lipoic acid. Experimental details for the synthesis and purification techniques of specific examples of molecules will be given. The synthesized molecules combine antioxidant activity with a variety of other biological activities such as protection against reperfusion arrhythmias, neuroprotective, and anti-inflammatory activity.
在一个分子支架中包含两个药效基团的杂化分子的设计与合成，是一种成熟的合成具有双重活性的更有效药物的方法。在本章中，我们将介绍我们用于制备含有“通用抗氧化剂”α-硫辛酸的杂化化合物的最重要的合成方法。将给出特定分子实例的合成和纯化技术的实验细节。合成的分子将抗氧化活性与多种其他生物活性相结合，如预防再灌注心律失常、神经保护和抗炎活性。
