Synthesis and biological evaluation, of unprecedented classes of spiro-β-lactams and azido-β-lactams as acyl-CoA:cholesterol acyltransferase inhibitors

被引:22
作者
Benfatti, Fides [1 ]
Cardillo, Giuliana [1 ]
Gentilucci, Luca [1 ]
Tolomelli, Alessandra [1 ]
机构
[1] Univ Bologna, Dipartimento Chim G Ciamician, I-40126 Bologna, Italy
关键词
Acyl-CoA cholesterol O-acyltransferase; beta-lactams; cholesterol absorption inhibition; azides; spiro derivatives;
D O I
10.1016/j.bmcl.2007.01.027
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Unprecedented classes of four- and five-membered hydroxyl-spiro-beta-lactams and hydroxyl-azido-beta-lactams were prepared via regioselective ring opening of hydroxyl-epoxides. The potential of these particular beta-lactams as biologically active compounds has been confirmed by the results obtained in ACAT inhibition assays. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1946 / 1950
页数:5
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