Abstract
A series of tryptamine derivatives with modified sulfonamide were designed, synthesized, and evaluated for their ability to stimulate cAMP accumulation in CHO cells expressing the cloned human beta3-adrenergic receptor (AR). For this series of compounds, our objective was to symmetrize the alpha-position of the tryptamine moiety maintaining its activity and reducing the cost of production. Compound 11h, having m-aminobenzene, exhibited excellent agonistic activity for beta3-AR with excellent subtype selectivity.
MeSH terms
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Adrenergic beta-3 Receptor Agonists*
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Adrenergic beta-Agonists / chemical synthesis*
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Adrenergic beta-Agonists / chemistry
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Adrenergic beta-Agonists / pharmacology
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Animals
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CHO Cells
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Cloning, Molecular
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Cricetinae
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Cyclic AMP / metabolism
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Drug Evaluation, Preclinical
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Humans
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Hydrocarbons
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Methane / analogs & derivatives*
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Methane / chemistry*
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Molecular Conformation
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry
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Sulfonamides / pharmacology
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Tryptamines / chemistry*
Substances
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Adrenergic beta-3 Receptor Agonists
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Adrenergic beta-Agonists
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Hydrocarbons
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Sulfonamides
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Tryptamines
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carbene
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Cyclic AMP
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Methane