Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines

Autor:	Richard Wynn, Brian Wayland, Ronald M. Klabe, Brent Douty, Andrew P. Combs, Eddy W. Yue, Min Wei, Lucie Gonneville, Paul J. Ala, Timothy Burn, Lori L. Bostrom, Michael J. Bower, Phillip Liu, James Russell Pruitt
Rok vydání:	2007
Předmět:	Models Molecular Stereochemistry Clinical Biochemistry Pharmaceutical Science Imidazoline derivatives Crystallography X-Ray Biochemistry Chemical synthesis Structure-Activity Relationship Drug Discovery Hydrolase Enzyme Inhibitors Imidazolines Molecular Biology chemistry.chemical_classification Protein Tyrosine Phosphatase Non-Receptor Type 1 biology Organic Chemistry Imidazoles Sulfonamide Thiazoles Enzyme chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine Isothiazolidinone
Zdroj:	Bioorganicmedicinal chemistry letters. 18(1)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2630cdf27b46ce4cb4099aed23de6264 https://pubmed.ncbi.nlm.nih.gov/18037290 Zobrazit plný text záznamu Full Text from ScienceDirect