Abstract
A series of thienopyrimidinone bis-aminopyrrolidine ureas were designed, synthesized, and evaluated for their ability to bind melanin-concentrating hormone receptor-1. These compounds exhibit potent binding affinity (K(i)=3 nM) and good in vitro metabolic stability.
MeSH terms
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Animals
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Chemistry, Pharmaceutical / methods*
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Cytochrome P-450 CYP2D6 Inhibitors
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Drug Design
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Humans
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Inhibitory Concentration 50
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Kinetics
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Mice
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Models, Chemical
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Molecular Conformation
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Protein Binding
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Pyrrolidines / chemistry*
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Receptors, Somatostatin / antagonists & inhibitors*
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Structure-Activity Relationship
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Urea / analogs & derivatives*
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Urea / chemistry*
Substances
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Cytochrome P-450 CYP2D6 Inhibitors
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MCHR1 protein, human
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Pyrrolidines
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Receptors, Somatostatin
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Urea