Novel 11[beta]-hydroxysteroid dehydrogenase 1 inhibitors reduce cortisol levels in keratinocytes and improve dermal collagen content in human ex vivo skin after exposure to cortisone and UV

• Published in: PloS one Vol. 12; no. 2; p. e0171079
• Main Authors: Boudon, Stéphanie M, Vuorinen, Anna, Geotti-Bianchini, Piero, Wandeler, Eliane, Kratschmar, Denise V, Heidl, Marc, Campiche, Remo, Jackson, Eileen, Odermatt, Alex
• Format: Journal Article
• Language: English
• Published: Public Library of Science 02.02.2017
• Subjects: Collagen; Health aspects; Hydrocortisone; Keratinocytes; Skin

Activity and selectivity assessment of new bi-aryl amide 11[beta]-hydroxysteroid dehydrogenase 1 (11[beta]-HSD1) inhibitors, prepared in a modular manner via Suzuki cross-coupling, are described. Several compounds inhibiting 11[beta]-HSD1 at nanomolar concentrations were identified. Compounds 2b, 3e...