为此,Renslo博士与其同事已经在分析并尝试修饰氨噻唑的分子结构,以使之能通过血脑屏障。
As they report in the Journal of Medicinal Chemistry, they think they have now pulled off thetrick.
根据他们在药物化学杂志的报道,他们已经找到了突破口。
They did it by removing groups of atoms called hydrogen-bond donors from the originalmolecules and adding a ring of carbon and hydrogen atoms.
他们移除氨噻唑分子上一组提供氢键的原子,并加上一个碳氢环。修饰后的氨噻唑分子看起来更像胆固醇分子。
That made the aminothiazoles look more like cholesterolwhich despite its malign everydayreputation is an important component of brains and routinely crosses the blood-brainbarrier.
尽管胆固醇整天被认为是个对人体有害的物质,但它却是脑的重要成分,是通过血脑屏障的常客。
It worked.
成功了!
When Dr Renslo fed mice a diet containing the improved aminothiazoles, he found that themost promising of them accumulated in the brain in concentrations nearly 25 times higherthan those required to clear prions from cultured cells.
Renslo博士给小鼠喂食含有改进后的氨噻唑的饮食后,发现这些最有希望的分子在小鼠的脑内聚集,其浓度达到清除体外培养细胞内朊病毒所需浓度的25倍。
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