4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 3. Identification of lead candidate.
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.
Wood
Jill
J
Bayer Research Center, Bayer HealthCare, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA.
Bagi
Cedo M
CM
Akuche
Christiana
C
Bacchiocchi
Antonietta
A
Baryza
Jeremy
J
Blue
Marie-Luise
ML
Brennan
Catherine
C
Campbell
Ann-Marie
AM
Choi
Soongyu
S
Cook
James H
JH
Conrad
Patricia
P
Dixon
Brian R
BR
Ehrlich
Paul P
PP
Gane
Todd
T
Gunn
David
D
Joe
Ted
T
Johnson
Jeffrey S
JS
Jordan
Jerold
J
Kramss
Richard
R
Liu
Peiying
P
Levy
Joan
J
Lowe
Derek B
DB
McAlexander
Ian
I
Natero
Reina
R
Redman
Anikó M
AM
Scott
William J
WJ
Town
Christopher
C
Wang
Ming
M
Wang
Yamin
Y
Zhang
Zhonghua
Z
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*
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