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Selective Reduction of Trigonellyl Group to the Corresponding Dihydropyridine in the Presence of Disulfide Group

机译:在二硫键存在下将三角烯基选择性还原为相应的二氢吡啶

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摘要

For many years, there has been considerable interest in the synthetic method, utility, and biological activity of various dihydropyridines.1 In recent years, based on the redox system, which is analogous to the endogenous NADH-NAD~+ system, we developed a chemical delivery system (CDS), using a dihydropyridine-pyridinium ion redox system for the specific delivery and sustained release of drug in the brain. In this CDS system, the biologically active compound linked to a lipoidal dihydropyridine carrier can crosses the BBB and is then oxidized to the pyridinium ion form in the brain, which is locked and retained in the brain because the increased hydrophilicity hinders BBB permeability (Figure 1).
机译:多年来,人们对各种二氢吡啶的合成方法,实用性和生物活性产生了浓厚的兴趣。1近年来,基于类似于内源性NADH-NAD〜+系统的氧化还原系统,我们开发了一种化学递送系统(CDS),使用二氢吡啶-吡啶鎓离子氧化还原系统对大脑中的药物进行特定的递送和持续释放。在此CDS系统中,与脂质二氢吡啶载体连接的生物活性化合物可以穿过血脑屏障,然后被氧化为大脑中的吡啶鎓离子形式,由于增加的亲水性阻碍了血脑屏障的通透性而被锁定并保留在脑中(图1 )。

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