title: 4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 3. Identification of lead candidate.
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.
authors.affiliation: Bayer Research Center, Bayer HealthCare, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA.
authors.forename: Jill
authors.initials: J
authors.lastname: Wood
authors.forename: Cedo M
authors.initials: CM
authors.lastname: Bagi
authors.forename: Christiana
authors.initials: C
authors.lastname: Akuche
authors.forename: Antonietta
authors.initials: A
authors.lastname: Bacchiocchi
authors.forename: Jeremy
authors.initials: J
authors.lastname: Baryza
authors.forename: Marie-Luise
authors.initials: ML
authors.lastname: Blue
authors.forename: Catherine
authors.initials: C
authors.lastname: Brennan
authors.forename: Ann-Marie
authors.initials: AM
authors.lastname: Campbell
authors.forename: Soongyu
authors.initials: S
authors.lastname: Choi
authors.forename: James H
authors.initials: JH
authors.lastname: Cook
authors.forename: Patricia
authors.initials: P
authors.lastname: Conrad
authors.forename: Brian R
authors.initials: BR
authors.lastname: Dixon
authors.forename: Paul P
authors.initials: PP
authors.lastname: Ehrlich
authors.forename: Todd
authors.initials: T
authors.lastname: Gane
authors.forename: David
authors.initials: D
authors.lastname: Gunn
authors.forename: Ted
authors.initials: T
authors.lastname: Joe
authors.forename: Jeffrey S
authors.initials: JS
authors.lastname: Johnson
authors.forename: Jerold
authors.initials: J
authors.lastname: Jordan
authors.forename: Richard
authors.initials: R
authors.lastname: Kramss
authors.forename: Peiying
authors.initials: P
authors.lastname: Liu
authors.forename: Joan
authors.initials: J
authors.lastname: Levy
authors.forename: Derek B
authors.initials: DB
authors.lastname: Lowe
authors.forename: Ian
authors.initials: I
authors.lastname: McAlexander
authors.forename: Reina
authors.initials: R
authors.lastname: Natero
authors.forename: Anikó M
authors.initials: AM
authors.lastname: Redman
authors.forename: William J
authors.initials: WJ
authors.lastname: Scott
authors.forename: Christopher
authors.initials: C
authors.lastname: Town
authors.forename: Ming
authors.initials: M
authors.lastname: Wang
authors.forename: Yamin
authors.initials: Y
authors.lastname: Wang
authors.forename: Zhonghua
authors.initials: Z
authors.lastname: Zhang
mesh_terms: D015067:17-Hydroxysteroid Dehydrogenases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D008252:Macaca fascicularis; D011760:Pyrrolidinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: C540795:5-(15-hydroxy(5-(3-pyridyl)(2-thienyl))methyl)-1-methyl-4-phenylpyrrolidin-2-one; D004791:Enzyme Inhibitors; D011760:Pyrrolidinones; D013876:Thiophenes; D015067:17-Hydroxysteroid Dehydrogenases; C044256:3 (or 17)-beta-hydroxysteroid dehydrogenase