4.5 Article

Synthesis of a series of novel 2,4,5-trisubstituted selenazole compounds as potential PLTP inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 17, Pages 5123-5125

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.017

Keywords

Atherosclerosis; PLTP inhibitor; 2,4,5-Trisubstituted selenazole

Funding

  1. National Nature Science Foundation of China [30701042]

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Based on a homology-modeled structure of PLTP and characteristic structural features of reported cholesteryl ester transfer protein (CETP) inhibitors, we designed and synthesized a novel series of 2,4,5-trisubstituted selenazole compounds. Biological evaluation reveals that compounds 12 and 17 exhibit favorable PLTP activity, and their IC(50)s are 8 mu M and 10 mu M, respectively. (C) 2010 Elsevier Ltd. All rights reserved.

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