Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors

A series of potent, selective sulfonylfuran urea endothelial lipase inhibitors is reported. Mechanism of action studies are also discussed. Endothelial lipase (EL) activity has been implicated in HDL catabolism, vascular inflammation, and atherogenesis, and inhibitors are therefore expected to be us...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009, Vol.19 (1), p.27-30
Hauptverfasser:	Goodman, Krista B., Bury, Michael J., Cheung, Mui, Cichy-Knight, Maria A., Dowdell, Sarah E., Dunn, Allison K., Lee, Dennis, Lieby, Jeffrey A., Moore, Michael L., Scherzer, Daryl A., Sha, Deyou, Suarez, Dominic P., Murphy, Dennis J., Harpel, Mark R., Manas, Eric S., McNulty, Dean E., Annan, Roland S., Matico, Rosalie E., Schwartz, Benjamin K., Trill, John J., Sweitzer, Thomas D., Wang, Da-yuan, Keller, Paul M., Krawiec, John A., Jaye, Michael C.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Cardiovascular Diseases - drug therapy Cardiovascular system Drug Discovery Drug Evaluation, Preclinical Endothelial lipase Endothelium - enzymology Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Furan Furans Humans Irreversible inhibitors Lipase - antagonists & inhibitors Medical sciences Miscellaneous Pharmacology. Drug treatments Phospholipases Selectivity Sulfonylurea Compounds - chemical synthesis Sulfonylurea Compounds - pharmacology
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