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

Cui Ling; Zhibing Zheng; Xian Cheng Jiang; Wu Zhong; Song Li

doi:10.1016/j.bmcl.2010.07.017

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

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5123-5. doi: 10.1016/j.bmcl.2010.07.017.

Authors

Cui Ling¹, Zhibing Zheng, Xian Cheng Jiang, Wu Zhong, Song Li

Affiliation

¹ Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing, PR China.

PMID: 20667734
DOI: 10.1016/j.bmcl.2010.07.017

Abstract

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 microM and 10 microM, respectively.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Azoles / chemistry*
Drug Evaluation, Preclinical
Inhibitory Concentration 50
Phospholipid Transfer Proteins / antagonists & inhibitors*
Selenium Compounds / chemical synthesis*
Selenium Compounds / chemistry
Selenium Compounds / pharmacology*

Substances

Azoles
Phospholipid Transfer Proteins
Selenium Compounds