Welsh School of Pharmacy, Cardiff University, Redwood Building, Cardiff CF10 3NB, Wales, UK.
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2200-3. doi: 10.1016/j.bmcl.2010.02.035. Epub 2010 Feb 13.
Orthoesters are acid-sensitive moieties that allow substantial structural diversity for biological applications including drug delivery. Here, the pH-sensitivity of a range of novel orthoester based compounds was compared in the range 7.5-4.5 that is characteristic of the increased acidification during endocytosis. We find that simple modifications close to the orthoester had major effects on both the rate and extent of hydrolysis, suggesting this could be exploited for activating drug delivery systems on endocytic pathways.
酯是一种对酸敏感的基团，它为包括药物传递在内的生物应用提供了广泛的结构多样性。在这里，在 7.5-4.5 的范围内比较了一系列新型酯基化合物的 pH 敏感性，这是内吞作用过程中酸度增加的特征。我们发现，靠近酯的简单修饰对水解的速率和程度有重大影响，这表明这可以用于激活内吞途径中的药物传递系统。
