Abstract
The synthesis and antiallergic activity of a series of novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles are described. A number of the compounds inhibit the release of histamine from anti-IgE stimulated basophils obtained from allergic donors. Optimal inhibition is exhibited in benzothiophenes with a 3-alkoxy substituent in combination with a 5-methoxy, 6-methoxy, or a 5,6-dimethoxy group. Compound 13c (CI-959) also inhibited respiratory burst of human neutrophils and the release of mediators from anti-IgE-stimulated human chopped lung.
MeSH terms
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Antibodies, Anti-Idiotypic / immunology
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Basophils / drug effects
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Basophils / immunology
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Basophils / physiology
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Benzofurans / chemical synthesis*
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Benzofurans / pharmacology
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Eosinophils / drug effects
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Eosinophils / physiology
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Histamine Antagonists / chemical synthesis*
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Histamine Antagonists / pharmacology
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Histamine Release / drug effects
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Humans
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Hypersensitivity / blood
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Immunoglobulin E / immunology
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Lung / drug effects
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Lung / metabolism
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Molecular Structure
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Naphthalenes / chemical synthesis*
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Naphthalenes / pharmacology
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Neutrophils / drug effects
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Neutrophils / physiology
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Respiratory Burst / drug effects
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Structure-Activity Relationship
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Tetrazoles / chemical synthesis*
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Tetrazoles / pharmacology
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Thiophenes / chemical synthesis*
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Thiophenes / pharmacology
Substances
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Antibodies, Anti-Idiotypic
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Benzofurans
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Histamine Antagonists
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Naphthalenes
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Tetrazoles
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Thiophenes
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CI 959
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Immunoglobulin E