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

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

Bioorg Med Chem Lett ; 16(18): 4965-8, 2006 Sep 15.

Article in English | MEDLINE | ID: mdl-16806919

ABSTRACT

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.

Subject(s)

17-Hydroxysteroid Dehydrogenases/antagonists & inhibitors , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Pyrrolidinones/chemistry , Pyrrolidinones/pharmacology , Thiophenes/chemistry , Thiophenes/pharmacology , 17-Hydroxysteroid Dehydrogenases/metabolism , Animals , Cell Line , Enzyme Inhibitors/chemistry , Humans , Inhibitory Concentration 50 , Macaca fascicularis , Pyrrolidinones/chemical synthesis , Rats , Stereoisomerism , Structure-Activity Relationship , Thiophenes/chemical synthesis

ABSTRACT

Subject(s)

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