期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 1, 页码 191-194出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.11.039
关键词
Farnesoid X receptor; Nuclear hormone receptors; Ugi-reaction; Benzimidazoles
Herein we describe the synthesis and structure activity relationship of a new class of FXR agonists identified from a high-throughput screening campaign. Further optimization of the original hits led to molecules that were highly active in an LDL-receptor KO model for dyslipidemia. The most promising candidate is discussed in more detail. (C) 2010 Elsevier Ltd. All rights reserved.
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