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17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog.
Gargano, Emanuele M Allegretta, Giuseppe Perspicace, Enrico Carotti, Angelo Van Koppen, Chris Frotscher, Martin Marchais-Oberwinkler, Sandrine Hartmann, Rolf W
Gargano, Emanuele M
Allegretta, Giuseppe
Perspicace, Enrico
Carotti, Angelo
Van Koppen, Chris
Frotscher, Martin
Marchais-Oberwinkler, Sandrine
Hartmann, Rolf W
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Abstract
Design and synthesis of a new class of inhibitors for the treatment of osteoporosis and its comparative h17β-HSD2 and m17β-HSD2 SAR study are described. 17a is the first compound to show strong inhibition of both h17β-HSD2 and m17β-HSD2, intracellular activity, metabolic stability, selectivity toward h17β-HSD1, m17β-HSD1 and estrogen receptors α and β as well as appropriate physicochemical properties for oral bioavailability. These properties make it eligible for pre-clinical animal studies, prior to human studies.
Citation
17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog. 2015, 10 (7):e0134754 PLoS ONE
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Article
Language
en
Description
Series/Report no.
ISSN
1932-6203