Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1

Autor:	Richard Friesen, Lynn Dufresne, Tom Y.-H. Wu, Denis Riendeau, Yves Ducharme, Joseph A. Mancini, Myriam Salem, Christine Brideau, Sébastien Guiral, Helene Juteau, Hugo Poirier
Rok vydání:	2010
Předmět:	medicine.medical_treatment Clinical Biochemistry Anti-Inflammatory Agents Pharmaceutical Science Isomerase Prostaglandin E synthase Biochemistry Dinoprostone Cell Line Mice Microsomes Drug Discovery medicine Animals Prostaglandin E2 Molecular Biology Prostaglandin-E Synthases chemistry.chemical_classification biology ATP synthase Chemistry Organic Chemistry Imidazoles In vitro High-Throughput Screening Assays Intramolecular Oxidoreductases Enzyme biology.protein Microsome Molecular Medicine lipids (amino acids peptides and proteins) Prostaglandin E medicine.drug
Zdroj:	Bioorganicmedicinal chemistry letters. 20(23)
ISSN:	1464-3405
Popis:	Microsomal prostaglandin E 2 synthase (mPGES-1) represents a potential target for novel analgesic and anti-inflammatory agents. High-throughput screening identified several leads of mPGES-1 inhibitors which were further optimized for potency and selectivity. A series of inhibitors bearing a biaryl imidazole scaffold exhibits excellent inhibition of PGE 2 production in enzymatic and cell-based assays. The synthesis of these molecules and their activities will be discussed.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de66c7f490f6be0a9ae9fb6b5c56b285 https://pubmed.ncbi.nlm.nih.gov/20965723 Zobrazit plný text záznamu Full Text from ScienceDirect