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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.

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 towar...

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Principais autores: Emanuele M Gargano, Giuseppe Allegretta, Enrico Perspicace, Angelo Carotti, Chris Van Koppen, Martin Frotscher, Sandrine Marchais-Oberwinkler, Rolf W Hartmann
Formato: Artigo
Idioma:Inglês
Publicado: Public Library of Science (PLoS) 2015-01-01
Series:PLoS ONE
Acceso en liña:http://europepmc.org/articles/PMC4521925?pdf=render
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