Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines

Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines

The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the i...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2008, Vol.18 (1), p.66-71
Hauptverfasser: Douty, Brent, Wayland, Brian, Ala, Paul J., Bower, Michael J., Pruitt, James, Bostrom, Lori, Wei, Min, Klabe, Ronald, Gonneville, Lucie, Wynn, Richard, Burn, Timothy C., Liu, Phillip C.C., Combs, Andrew P., Yue, Eddy W.
Format: Artikel
Sprache:eng
Schlagworte:
Biological and medical sciences
Crystallography, X-Ray
Drug Design
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
General and cellular metabolism. Vitamins
Imidazoles - chemical synthesis
Imidazoles - chemistry
Imidazoles - pharmacology
Imidazolines - chemical synthesis
Imidazolines - chemistry
Imidazolines - pharmacology
Isothiazolidinone
Medical sciences
Models, Molecular
Pharmacology. Drug treatments
Phosphotyrosine
Protein tyrosine phosphatase
Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors
PTP1B
Structure-Activity Relationship
Thiazoles - chemical synthesis
Thiazoles - chemistry
Thiazoles - pharmacology
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Zusammenfassung:The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are interacting extensively with the B site of the enzyme.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.11.012