Mevalonolactone derivatives as inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase.
作者:AIYA SATO、HIROSHI NOGUCHI、SEIJI MITSUI、ISAO KANEKO、YOKO SHIMADA
DOI:10.1248/cpb.28.1509
日期:——
Mevalonolactone derivatives were prepared via stereo-and regioselective bromolactonization of γ, δ-unsaturated acids and their structure-activity relationship in connection with their inhibitory activity in vitro against 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase, a rate-limiting enzyme in cholesterol biosynthesis, was investigated.
通过对γ, δ-不饱和酸进行立体选择性和区域选择性的溴内酯化反应制备了美瓦龙内酯衍生物,并研究了它们在体外对3-羟基-3-甲基谷氨酰辅酶A(HMG CoA)还原酶的抑制活性与其结构-活性关系,该酶是胆固醇生物合成中的限速酶。