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  • 4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 3. Identification of lead candidate.

4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 3. Identification of lead candidate.

Bioorganic & medicinal chemistry letters (2006-06-30)
Jill Wood, Cedo M Bagi, Christiana Akuche, Antonietta Bacchiocchi, Jeremy Baryza, Marie-Luise Blue, Catherine Brennan, Ann-Marie Campbell, Soongyu Choi, James H Cook, Patricia Conrad, Brian R Dixon, Paul P Ehrlich, Todd Gane, David Gunn, Ted Joe, Jeffrey S Johnson, Jerold Jordan, Richard Kramss, Peiying Liu, Joan Levy, Derek B Lowe, Ian McAlexander, Reina Natero, Anikó M Redman, William J Scott, Christopher Town, Ming Wang, Yamin Wang, Zhonghua Zhang
RESUMEN

A series of 4,5-disubstituted cis-pyrrolidinones was investigated as inhibitors of 17beta-HSD II for the treatment of osteoporosis. Biochemical data for several compounds are given. Compound 42 was selected as the lead candidate.

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Phenylpropiolic acid, 99%