Abstract

An ecofriendly effective synthetic reaction pathway has been developed for the synthesis of phosphoramidates under mild reaction conditions. This is a green procedure and can be used in drug discovery for the synthesis of phosphoramidate intermediates used as prodrugs to enhance therapeutic potential properties of the parent drugs. All the title compounds are docked with α-amylase and also tested for in vitro α-amylase activity. All the synthesized compounds (3a–h) have exhibited higher in vitro α-amylase inhibitory activity than the standard acarbose, with 3f, 3g and 3h showing the better activity. The docking results are in good agreement with the in vitro α-amylase inhibitory activity. Interestingly aromatic phosphites have shown good activity when compared with aliphatic phosphites.

抽象的

已经开发了在温和的反应条件下合成氨基磷酸酯的生态友好的有效合成反应途径。这是一种绿色程序，可用于药物发现中，以合成用作前药的氨基磷酸酯中间体，以增强母体药物的治疗潜能。所有标题化合物都与α-淀粉酶对接，并测试了体外α-淀粉酶的活性。所有合成的化合物（3a–h）均具有比标准阿卡波糖更高的体外α-淀粉酶抑制活性，其中3f，3g和3h表现出更好的活性。对接结果与体外α-淀粉酶抑制活性。有趣的是，与脂族亚磷酸酯相比，芳族亚磷酸酯显示出良好的活性。