Abstract
A series of novel pyrazole carboxamides is disclosed that demonstrate strong immunosuppressant activity in rodent and human mixed leukocyte response (MLR) assays (IC50 < 1 microM). The synthesis, biological activity, mode of action, and pharmacokinetic properties of this new lead series are discussed.
MeSH terms
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Animals
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Biological Availability
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Humans
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Immunosuppressive Agents / chemical synthesis*
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Immunosuppressive Agents / pharmacokinetics
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Immunosuppressive Agents / pharmacology*
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Isoxazoles / pharmacology
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Leflunomide
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Lymphocyte Activation / drug effects
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Lymphocyte Culture Test, Mixed
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Pyrazoles / chemical synthesis*
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Pyrazoles / pharmacokinetics
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Pyrazoles / pharmacology*
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Rats
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Structure-Activity Relationship
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T-Lymphocytes / drug effects
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T-Lymphocytes / immunology
Substances
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Immunosuppressive Agents
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Isoxazoles
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Pyrazoles
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Leflunomide