Abstract
The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki = 1 nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Inhibitory Concentration 50
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Molecular Structure
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Pyrrolidines / chemical synthesis
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Pyrrolidines / chemistry*
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Pyrrolidines / pharmacokinetics
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Pyrrolidines / pharmacology*
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Rats
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Receptors, Somatostatin / antagonists & inhibitors*
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Receptors, Somatostatin / metabolism
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Structure-Activity Relationship
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Urea / analogs & derivatives*
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Urea / chemical synthesis
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Urea / chemistry
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Urea / pharmacokinetics
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Urea / pharmacology
Substances
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MCHR1 protein, rat
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Pyrrolidines
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Receptors, Somatostatin
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bis-aminopyrrolidine urea
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Urea