Sunazuka T, Tsuzuki K, Kumagai H, Tomoda H, Tanaka H, Nagashima H, Hashizume H, Omura S
Research Center for Biological Function, Kitasato Institute, Tokyo, Japan.
J Antibiot (Tokyo). 1992 Jul;45(7):1139-47. doi: 10.7164/antibiotics.45.1139.
Simple and efficient syntheses of 1233A analogs were developed and the inhibitory activity of the analogs against hydroxymethylglutaryl coenzyme A (HMG-CoA) synthase was determined. Study of the structure-activity relationships revealed that not only the geometry in beta-lactone moiety but also the length of the carbon side chain is important for inhibitory activity against HMG-CoA synthase.
开发了1233A类似物的简单高效合成方法，并测定了这些类似物对羟甲基戊二酰辅酶A（HMG-CoA）合酶的抑制活性。构效关系研究表明，不仅β-内酯部分的几何结构，而且碳侧链的长度对HMG-CoA合酶的抑制活性都很重要。
