新型2-吡啶酮肽模拟物法呢基蛋白酶2/3抑制剂的设计与合成

Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors.

作者信息

Verissimo Edite, Berry Neil, Gibbons Peter, Cristiano M Lurdes S, Rosenthal Philip J, Gut Jiri, Ward Stephen A, O'Neill Paul M

机构信息

Department of Chemistry, Biochemistry and Pharmacy, and CCMAR, University of Algarve, Campus de Gambelas, Faro 8005-039, Portugal.

出版信息

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4210-4. doi: 10.1016/j.bmcl.2008.05.068. Epub 2008 May 20.

DOI:10.1016/j.bmcl.2008.05.068

PMID:18554905

Abstract

The structure-based design, chemical synthesis and in vitro activity evaluation of various falcipain inhibitors derived from 2-pyridone are reported. These compounds contain a peptidomimetic binding determinant and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site.

摘要

报道了基于结构设计、化学合成以及对源自2-吡啶酮的各种疟原虫蛋白酶抑制剂的体外活性评估。这些化合物含有一个拟肽结合决定簇和一个能够使半胱氨酸蛋白酶活性位点失活的迈克尔受体末端部分。