Venier, O.; Pascal, C.; Braun, A.; Namane, C.; Mougenot, P.; Crespin, O.; Pacquet, F.; Mougenot, C.; Monseau, C.; Onofri, B.; Dadji-Faihun, R.; Leger, C.; Ben-Hassine, M.; Van-Pham, T.; Ragot, J.L.; Philippo, C.; Gussregen, S.; Engel, C.; Farjot, G.; Noah, L.; Maniani, K.; Nicolai, E.: Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11beta-hydroxysteroid-dehydrogenase type 1. Bioorganic & Medicinal Chemistry Letters 21 (2011), p. 2244-2251
10.1016/j.bmcl.2011.02.111
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.