title: Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1.
abstract: 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.
authors: Sanofi-aventis R&D, 1 Avenue Pierre Brossolette, 91385 Chilly-Mazarin, France. Olivier.Venier@sanofi-aventis.com
authors: Olivier
authors: O
authors: Venier
authors: Cécile
authors: C
authors: Pascal
authors: Alain
authors: A
authors: Braun
authors: Claudie
authors: C
authors: Namane
authors: Patrick
authors: P
authors: Mougenot
authors: Olivier
authors: O
authors: Crespin
authors: François
authors: F
authors: Pacquet
authors: Cécile
authors: C
authors: Mougenot
authors: Catherine
authors: C
authors: Monseau
authors: Bénédicte
authors: B
authors: Onofri
authors: Rommel
authors: R
authors: Dadji-Faïhun
authors: Céline
authors: C
authors: Leger
authors: Majdi
authors: M
authors: Ben-Hassine
authors: Thao
authors: T
authors: Van-Pham
authors: Jean-Luc
authors: JL
authors: Ragot
authors: Christophe
authors: C
authors: Philippo
authors: Stefan
authors: S
authors: Güssregen
authors: Christian
authors: C
authors: Engel
authors: Géraldine
authors: G
authors: Farjot
authors: Lionel
authors: L
authors: Noah
authors: Karima
authors: K
authors: Maniani
authors: Eric
authors: E
authors: Nicolaï
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000284:Administration, Oral; D000818:Animals; D001665:Binding Sites; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D057166:High-Throughput Screening Assays; D006801:Humans; D051379:Mice; D011720:Pyrazoles / Q000737:chemistry*; D011759:Pyrrolidines / Q000737:chemistry*; D014508:Urea / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D004791:Enzyme Inhibitors; D011720:Pyrazoles; D011759:Pyrrolidines; C031280:pyrazole; D014508:Urea; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; C032519:pyrrolidine