Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372490 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
A series of 2-arylbenzoxazole inhibitors of the cholesterol ester transfer protein (CETP) is described. Structure–activity studies focused on variation of the substitution of the benzoxazole moiety. Substitution at the 5- and 7-positions of the benzoxazole moiety was found to be beneficial for CETP inhibition. Compound 47 was found to be the most potent inhibitor in this series and inhibited CETP with an IC50 of 28 nM.
Graphical abstractCompound 47 was found to be a potent inhibitor of CETP and had an IC50 of 28 nM.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Cameron J. Smith, Amjad Ali, Liya Chen, Milton L. Hammond, Matt S. Anderson, Ying Chen, Suzanne S. Eveland, Qiu Guo, Sheryl A. Hyland, Denise P. Milot, Carl P. Sparrow, Samuel D. Wright, Peter J. Sinclair,