Abstract
The synthesis of a series of carbazole derivatives and their SAR at the NPY Y1 receptor is described. Modulation of physicochemical properties by appropriate decoration led to the identification of a high-affinity NPY Y1 antagonist that shows high brain penetration and modest oral bioavailability.
MeSH terms
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Animals
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Biological Availability
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Brain / drug effects
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Brain / metabolism
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CHO Cells
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Carbazoles / chemical synthesis*
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Carbazoles / pharmacokinetics
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Carbazoles / pharmacology*
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Chemical Phenomena
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Chemistry, Physical
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Cricetinae
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Cricetulus
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Half-Life
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Indicators and Reagents
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Male
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Rats
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Rats, Sprague-Dawley
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Receptors, Neuropeptide Y / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Carbazoles
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Indicators and Reagents
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Receptors, Neuropeptide Y
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neuropeptide Y-Y1 receptor