PLoS ONE (2015)
Update date:2022-08-02
Topics:
Gargano, Emanuele M.
Allegretta, Giuseppe
Perspicace, Enrico
Carotti, Angelo
Van Koppen, Chris
Frotscher, Martin
Marchais-Oberwinkler, Sandrine
Hartmann, Rolf W.
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. Copyright:
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