4.5 Article

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

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 14, 页码 4210-4214

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.05.068

关键词

malaria; Plasmodium falciparum; cysteine protease; falcipain-2; peptidomimetic

资金

  1. Biotechnology and Biological Sciences Research Council [BB/C006321/1] Funding Source: Medline
  2. Biotechnology and Biological Sciences Research Council [BB/C006321/1] Funding Source: researchfish

向作者/读者索取更多资源

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. (C) 2008 Elsevier Ltd. All rights reserved.

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