Abstract
Novel tetrahydrodiazabenzazulene derivatives, designed from the lead compound 1 discovered by screening of our in-house chemical library, were prepared and found to be potent neuropeptide Y-Y5 (NPY-Y5) receptor antagonists. The structure-activity relationships are described. Compounds 7 (FR240662) and 16 (FR252384) were especially attractive owing to their high affinities for the NPY-Y5 receptors, oral absorption and permeability to brain.
MeSH terms
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Administration, Oral
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Animals
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Azulenes
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Benzoic Acid / chemistry
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Binding Sites
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Brain / drug effects
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Brain / metabolism
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Cycloheptanes / chemical synthesis*
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Cycloheptanes / chemistry
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Cycloheptanes / pharmacology*
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Eating
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Heterocyclic Compounds / chemical synthesis
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Heterocyclic Compounds / pharmacology
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Models, Molecular
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Permeability / drug effects
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Rats
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Rats, Zucker
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Receptors, Neuropeptide Y / antagonists & inhibitors*
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Receptors, Neuropeptide Y / metabolism
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Structure-Activity Relationship
Substances
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Azulenes
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Cycloheptanes
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Heterocyclic Compounds
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Receptors, Neuropeptide Y
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neuropeptide Y5 receptor
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azulene
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Benzoic Acid