Vaccaro W D, Sher R, Davis H R
Schering-Plough Research Institute, Kenilworth, New Jersey 07033-0539, USA.
Bioorg Med Chem Lett. 1998 Feb 3;8(3):319-22. doi: 10.1016/s0960-894x(98)00009-2.
Metabolism initiated SAR studies led to the discovery of a new class of potent 2-azetidinone cholesterol absorption inhibitors. These studies found that a heteroatom at the para position of the C-4 phenyl ring is not a requirement for cholesterol absorption inhibition as was suggested by earlier findings. Substitution of Ph-linker-COOR for PhOMe at the C-4 position enhanced cholesterol absorption inhibition.
基于代谢的构效关系（SAR）研究导致发现了一类新型强效2-氮杂环丁烷酮胆固醇吸收抑制剂。这些研究发现，如早期研究所表明的，C-4苯环对位的杂原子并非胆固醇吸收抑制所必需的。在C-4位用Ph-连接基-COOR取代PhOMe可增强胆固醇吸收抑制作用。
