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.
MeSH terms
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17-Hydroxysteroid Dehydrogenases / antagonists & inhibitors*
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17-Hydroxysteroid Dehydrogenases / metabolism
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Animals
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Cell Line
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Humans
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Inhibitory Concentration 50
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Macaca fascicularis
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Pyrrolidinones / chemical synthesis
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Pyrrolidinones / chemistry*
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Pyrrolidinones / pharmacology*
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Rats
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Stereoisomerism
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Structure-Activity Relationship
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Thiophenes / chemical synthesis
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Thiophenes / chemistry*
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Thiophenes / pharmacology*
Substances
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5-(15-hydroxy(5-(3-pyridyl)(2-thienyl))methyl)-1-methyl-4-phenylpyrrolidin-2-one
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Enzyme Inhibitors
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Pyrrolidinones
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Thiophenes
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17-Hydroxysteroid Dehydrogenases
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3 (or 17)-beta-hydroxysteroid dehydrogenase