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通过立体和区域选择性环氧开环合成叠氮基和氮丙啶基羟基β-内酰胺及其生物学评价。

Synthesis and biological evaluation of azido- and aziridino-hydroxyl-beta-lactams through stereo- and regioselective epoxide ring opening.

作者信息

Benfatti Fides, Cardillo Giuliana, Gentilucci Luca, Perciaccante Rossana, Tolomelli Alessandra, Catapano Alberico

机构信息

Department of Chemistry "G. Ciamician", University of Bologna, Via Selmi 2, 40126 Bologna, Italy.

出版信息

J Org Chem. 2006 Nov 24;71(24):9229-32. doi: 10.1021/jo0615652.

Abstract

Two new classes of azido- and aziridino-hydroxyl-beta-lactam containing structures have been prepared by means of a stereo- and regioselective epoxide ring opening. The straightforwardness of the procedure makes this strategy useful for the synthesis of potentially bioactive compounds. Some selected examples showed promising activity in acyl CoA-cholesterol acyltransferase inhibition assays.

摘要

通过立体和区域选择性环氧开环反应制备了两类新的含叠氮基和氮丙啶基的羟基-β-内酰胺结构。该方法的简便性使得该策略对于合成潜在生物活性化合物很有用。一些选定的例子在酰基辅酶A-胆固醇酰基转移酶抑制试验中显示出有前景的活性。

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