Bioorganic & medicinal chemistry letters, 2011-04, Vol.21 (8), p.2244-2251
- Venier, Olivier
- Pascal, Cécile
- Braun, Alain
- Namane, Claudie
- Mougenot, Patrick
- Crespin, Olivier
- Pacquet, François
- Mougenot, Cécile
- Monseau, Catherine
- Onofri, Bénédicte
- Dadji-Faïhun, Rommel
- Leger, Céline
- Ben-Hassine, Majdi
- Van-Pham, Thao
- Ragot, Jean-Luc
- Philippo, Christophe
- Güssregen, Stefan
- Engel, Christian
- Farjot, Géraldine
- Noah, Lionel
- Maniani, Karima
- Nicolaï, Eric
2011
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- Autor(en) / Beteiligte
- Venier, Olivier
- Pascal, Cécile
- Braun, Alain
- Namane, Claudie
- Mougenot, Patrick
- Crespin, Olivier
- Pacquet, François
- Mougenot, Cécile
- Monseau, Catherine
- Onofri, Bénédicte
- Dadji-Faïhun, Rommel
- Leger, Céline
- Ben-Hassine, Majdi
- Van-Pham, Thao
- Ragot, Jean-Luc
- Philippo, Christophe
- Güssregen, Stefan
- Engel, Christian
- Farjot, Géraldine
- Noah, Lionel
- Maniani, Karima
- Nicolaï, Eric
- Titel
- Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2011-04, Vol.21 (8), p.2244-2251
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2011
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2011.02.111Titel-ID: cdi_proquest_miscellaneous_872140547
- Format
- –
- Schlagworte
- 11-beta-Hydroxysteroid Dehydrogenase Type 1 - antagonists & inhibitors, 11-beta-Hydroxysteroid Dehydrogenase Type 1 - metabolism, 11β-HSD-1 inhibitors, 11β-Hydroxysteroid-dehydrogenase type 1, Administration, Oral, Animals, Binding Sites, Biological and medical sciences, chemistry, Crystallography, X-Ray, Enzyme Inhibitors - chemical synthesis, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacokinetics, General and cellular metabolism. Vitamins, High-Throughput Screening Assays, Humans, Medical sciences, Metabolic syndrome, Mice, Pharmacodynamic ex vivo assay, Pharmacology. Drug treatments, Pyrazoles - chemistry, Pyrrolidine-pyrazole, Pyrrolidines - chemistry, screening, Urea, Urea - chemical synthesis, Urea - chemistry, Urea - pharmacokinetics