Abstract
The continued SAR investigation of tryptamine-based human beta(3)-adrenergic receptor (AR) agonists is reported. Prior efforts resulted in the identification of 2 as a potent beta(3)-AR agonist. Further modification of the left side arylsulfonamide portion in 2 provided compounds with good cell permeability, which have potent agonistic activity for beta(3)-AR. Cinnamylamine analog 16i exhibited an excellent agonistic profile in vitro and good oral bioavailability in rats.
MeSH terms
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Administration, Oral
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Adrenergic Agonists / chemical synthesis*
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Adrenergic Agonists / pharmacokinetics*
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Adrenergic Agonists / pharmacology
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Biological Availability
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Cell Membrane Permeability
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Humans
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Inhibitory Concentration 50
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Receptors, Adrenergic, beta-3 / metabolism*
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / pharmacokinetics
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Sulfonamides / pharmacology
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Tryptamines*
Substances
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Adrenergic Agonists
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Receptors, Adrenergic, beta-3
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Sulfonamides
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Tryptamines
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tryptamine