Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1

Autor:	Jean-Luc Ragot, Catherine Monseau, Cecile Pascal, Alain Braun, Lionel Noah, Thao Van-Pham, Rommel Dadji-Faïhun, Majdi Ben-Hassine, Olivier Venier, Géraldine Farjot, Patrick Mougenot, Eric Nicolai, Claudie Namane, Christophe Philippo, Olivier Crespin, Cécile Mougenot, Bénédicte Onofri, Stefan Gussregen, Karima Maniani, Christian Engel, François Pacquet, Céline Leger
Rok vydání:	2011
Předmět:	Pyrrolidines Clinical Biochemistry Administration Oral Pharmaceutical Science Pyrazole Crystallography X-Ray Biochemistry Chemical synthesis Pyrrolidine Mice chemistry.chemical_compound 11β-hydroxysteroid dehydrogenase type 1 11-beta-Hydroxysteroid Dehydrogenase Type 1 Drug Discovery Animals Humans Urea Enzyme Inhibitors Binding site Molecular Biology ADME chemistry.chemical_classification Binding Sites biology Organic Chemistry High-Throughput Screening Assays Enzyme chemistry biology.protein Pyrazoles Molecular Medicine hormones hormone substitutes and hormone antagonists Ex vivo
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:2244-2251
ISSN:	0960-894X
Popis:	A High Throughput Screening campaign allowed the identification of a novel class of ureas as 11β-HSD1 inhibitors. Rational chemical optimization provided potent and selective inhibitors of both human and murine 11β-HSD1 with an appropriate ADME profile and ex vivo activity in target tissues.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a453306e9f16edd9c82b584b9c9e2ff5 https://doi.org/10.1016/j.bmcl.2011.02.111 Zobrazit plný text záznamu Full Text from ScienceDirect