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Bioorg Med Chem Lett. 2013 May 1;23(9):2595-7. doi: 10.1016/j.bmcl.2013.02.113. Epub 2013 Mar 7.

A thiocarbamate inhibitor of endothelial lipase raises HDL cholesterol levels in mice.

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Janssen Research and Development, LLC, Welsh and McKean Roads, PO Box 776, Spring House, PA 19477, USA.


By screening directed libraries of serine hydrolase inhibitors using the cell surface form of endothelial lipase (EL), we identified a series of carbamate-derived (EL) inhibitors. Compound 3 raised plasma HDL-C levels in the mouse, and a correlation was found between HDL-C and plasma compound levels. Spectroscopic and kinetic studies support a covalent mechanism of inhibition. Our findings represent the first report of EL inhibition as an effective means for increasing HDL-C in an in vivo model.

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