Abstract
A previously discovered DHODH inhibitor series was further improved by replacing the cyclopentene ring by aromatic heterocycles. Different isomers of these compounds were prepared by the directed ortho-metallation procedure. The compounds are more active than the corresponding cyclopentene analogs and show potent effects on PBMC's proliferation.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Biphenyl Compounds / chemical synthesis
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Biphenyl Compounds / chemistry
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Biphenyl Compounds / pharmacology*
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Carbamates / chemical synthesis
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Carbamates / chemistry
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Carbamates / pharmacology*
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Carboxylic Acids / chemical synthesis
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Carboxylic Acids / chemistry
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Carboxylic Acids / pharmacology*
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Dihydroorotate Dehydrogenase
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Drug Design
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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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Molecular Structure
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Oxidoreductases Acting on CH-CH Group Donors / antagonists & inhibitors*
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Quantitative Structure-Activity Relationship
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Recombinant Proteins / antagonists & inhibitors
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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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Biphenyl Compounds
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Carbamates
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Carboxylic Acids
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Dihydroorotate Dehydrogenase
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Enzyme Inhibitors
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Recombinant Proteins
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Thiophenes
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Oxidoreductases Acting on CH-CH Group Donors