Aminopyrrolidineamide inhibitors of site-1 protease

A series of aminopyrrolidineamide inhibitors of sterol regulatory element binding protein site-1 protease was identified. The discovery and efficacy of a series of potent aminopyrrolidineamide-based inhibitors of sterol regulatory element binding protein site-1 protease is described.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-08, Vol.17 (16), p.4411-4414
Main Authors: Hay, Bruce A., Abrams, Barbara, Zumbrunn, Allice Y., Valentine, James J., Warren, Laurie C., Petras, Stephen F., Shelly, Lorraine D., Xia, Angela, Varghese, Alison H., Hawkins, Julie L., Van Camp, Jennifer A., Robbins, Michael D., Landschulz, Katherine, Harwood, H. James
Format: Article
Language:English
Subjects:
Active Transport, Cell Nucleus - drug effects
Animals
Biological and medical sciences
Combinatorial Chemistry Techniques
Gene Expression Regulation
General and cellular metabolism. Vitamins
Humans
Hypolipidemic Agents - chemistry
Hypolipidemic Agents - pharmacology
Inhibitory Concentration 50
Male
Medical sciences
Metabolic syndrome
Mice
Molecular Structure
Pharmacology. Drug treatments
Proprotein Convertases - antagonists & inhibitors
Pyrroles - chemistry
Pyrroles - pharmacology
Serine Endopeptidases
Site-1 protease
SREBP
Sterol regulatory element binding protein
Sterol Regulatory Element Binding Proteins - metabolism
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Description
Summary:A series of aminopyrrolidineamide inhibitors of sterol regulatory element binding protein site-1 protease was identified. The discovery and efficacy of a series of potent aminopyrrolidineamide-based inhibitors of sterol regulatory element binding protein site-1 protease is described.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.06.031