PDF(Pubmed)
Abstract：
Like most phosphinic acids, the potent and selective RXP03 inhibitor of different MMPs exhibited moderate absorption and low bioavailability, which impaired its use. In an unprecedented attempt, we present an interesting synthetic approach to a new class of phosphinate prodrug, glycosyl ester of RXP03, to provide a potentially improved blood-brain barrier (BBB) behavior compared to the former lead compound RXP03. To validate this speculation, a predictive study for permeability enhancer of glycosyl ester of RXP03 showed encouraging insights to improve drug delivery across biological barriers.
摘要：
像大多数次膦酸一样，不同MMPs的有效和选择性RXP03抑制剂表现出中等吸收和低生物利用度，这损害了它的使用。在前所未有的尝试中，我们提出了一种新的次膦酸前药的有趣的合成方法，RXP03的糖基酯,以提供与前先导化合物RXP03相比潜在改善的血脑屏障(BBB)行为。为了验证这种猜测，一项针对RXP03糖基酯的渗透性增强剂的预测性研究显示出令人鼓舞的见解，可以改善跨生物屏障的药物递送。
