Design and synthesis of new hypocholesterolemic organosilanes with antioxidant properties
作者:J.-P. Gotteland、A. Delhon、D. Junquéro、P. Oms、S. Halazy
DOI:10.1016/0960-894x(96)00063-7
日期:1996.3
(Arylamino)methylsilane derivatives 3 have been prepared and identified as potent inhibitors of human LDL oxidation mediated by copper(II). Combination of this property with the structural requirement of squalene epoxidase inhibitors led to the design and synthesis of the (arylamino)methylsilane derivative 4 which was characterised as the first potent, orally active squalene epoxidase inhibitor with antioxidant properties.
(芳氨基)甲基硅烷衍生物3已被制备并鉴定为由铜(II)介导的人类LDL氧化的强效抑制剂。将这一特性与羊毛甾醇环氧酶抑制剂的结构要求相结合,设计并合成了(芳氨基)甲基硅烷衍生物4,其特征为首个强效、口服有效的羊毛甾醇环氧酶抑制剂,且具有抗氧化特性。