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β-羧乙基锗倍半氧化物(即Gc-132)是具广谱药理活性的水溶性有机锗化合物,但因其在体内代谢速度太快而影响药物利用度。因此,对它的各种衍生物的合成和生物活性研究受到重视。为提高Ge-132的亲脂性,增强药物活性,我们在分子中引入具有生物活性的氨基酸或杂环胺,合成了8种新型酰胺衍生物。合成路线如下:
Beta-carboxyethylgermanium sesquioxide (ie, Gc-132) is a water-soluble organogermanium compound with a broad spectrum of pharmacological activities, but its drug availability is affected by its in vivo metabolic rate. Therefore, its synthesis and biological activity of various derivatives of attention. In order to improve the lipophilicity of Ge-132 and enhance the activity of the drug, we introduced eight bioactive amino acids or heterocyclic amines into the molecule and synthesized eight novel amide derivatives. The synthetic route is as follows: