Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines

Autor:	Jakub Majer, Łukasz Bojarski, Katarzyna Bazydlo, Filip Stefaniak, Maciej Wieczorek, Damian Smuga, Rafał Moszczyński-Pętkowski, Malgorzata Borkowska, Sylwia Janowska, Krzysztof Dubiel, Mikołaj Matłoka
Rok vydání:	2018
Předmět:	Pyrimidine Stereochemistry 010402 general chemistry 01 natural sciences law.invention Structure-Activity Relationship chemistry.chemical_compound law Drug Discovery Pyridine Humans Structure–activity relationship Molecule Enzyme Inhibitors Pharmacology chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure Phosphoric Diester Hydrolases 010405 organic chemistry Organic Chemistry General Medicine Metabolic stability Recombinant Proteins 0104 chemical sciences Pyrimidines Enzyme chemistry 3' 5'-Cyclic-AMP Phosphodiesterases Recombinant DNA PDE10A
Zdroj:	European Journal of Medicinal Chemistry. 155:96-116
ISSN:	0223-5234
DOI:	10.1016/j.ejmech.2018.05.043
Popis:	New compounds containing [1,2,4]triazolo [1,5-a]pyridine (I), pyrazolo [1,5-a]pyridine (II), 1H-1,3-benzodiazole (III) and imidazo [1,2-a]pyrimidine (IV) backbones were designed and synthesized for PDE10A interaction. Among these compounds, 1H-1,3-benzodiazoles and imidazo [1,2-a]pyrimidines showed the highest affinity for PDE10A enzyme as well as good metabolic stability. Both classes of compounds were identified as selective and potent PDE10A enzyme inhibitors.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed6693497e82157aeeaa776658d7ba9c https://doi.org/10.1016/j.ejmech.2018.05.043 Zobrazit plný text záznamu Full Text from ScienceDirect