Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors

被引:27
作者
Burnett, DA [1 ]
Caplen, MA [1 ]
Domalski, MS [1 ]
Browne, ME [1 ]
Davis, HR [1 ]
Clader, JW [1 ]
机构
[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA
关键词
D O I
10.1016/S0960-894X(01)00750-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The discoveries of Sch 48461 and Sch 58235 and their novel pharmacology of inhibition of cholesterol absorption have prompted efforts to determine their biological mechanism of action (MOA). To this end, a series of radioiodinated analogues with good to excellent in vivo activity have been designed and synthesized as single enantiomers. They are structurally consistent with the allowable SAR of the 2-azetidinone class of cholesterol absorption inhibitors. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:311 / 314
页数:4
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