Abstract
In the course of our studies on retinoic acid receptor (RAR) agonists, we have designed and synthesized a series of benzofuran and benzothiophene derivatives. Some of these compounds (1a,b,e,f,j) markedly inhibited LPS-induced B-lymphocyte proliferation and exerted RARalpha selectivity. One of them, 4-[5-(4,7-dimethylbenzofuran-2-yl)pyrrol-2-yl]benzoic acid (1b), when orally administered significantly inhibited mouse antibody production and delayed type hypersensitivity (DTH) responses from a dose of 0.1 mg/kg.
MeSH terms
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Administration, Oral
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Animals
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Antibody Formation / drug effects
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B-Lymphocytes / cytology
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B-Lymphocytes / drug effects*
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Cell Division / drug effects
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Escherichia coli
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Female
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Furans / chemical synthesis*
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Furans / chemistry
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Furans / pharmacology
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Hypersensitivity, Delayed / drug therapy
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Immunosuppressive Agents / chemical synthesis*
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Immunosuppressive Agents / chemistry
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Immunosuppressive Agents / pharmacology
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In Vitro Techniques
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Lipopolysaccharides
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Mice
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Mice, Inbred BALB C
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Pyrroles / chemical synthesis*
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Pyrroles / chemistry
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Pyrroles / pharmacology
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Receptors, Retinoic Acid / agonists*
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Retinoic Acid Receptor alpha
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Structure-Activity Relationship
Substances
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Furans
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Immunosuppressive Agents
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Lipopolysaccharides
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Pyrroles
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Rara protein, mouse
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Receptors, Retinoic Acid
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Retinoic Acid Receptor alpha
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ER 38925