Abstract
This paper describes the lead optimization of a new series of potent, selective, orally bioavailable, brain-penetrant MCH-1 receptor antagonists. A major focus of the work was to achieve a selectivity profile appropriate for in vivo efficacy studies and safety.
MeSH terms
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Amides / chemistry
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Amides / pharmacokinetics
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Amides / pharmacology
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Animals
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacokinetics
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Benzimidazoles / pharmacology
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Crystallography, X-Ray
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Humans
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Indans / chemistry
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Indans / pharmacokinetics
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Indans / pharmacology*
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Kinetics
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Piperidines / chemistry
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Piperidines / pharmacokinetics
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Piperidines / pharmacology
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Rats
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Rats, Sprague-Dawley
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Receptors, Somatostatin / antagonists & inhibitors*
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Receptors, Somatostatin / chemistry
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Receptors, Somatostatin / metabolism
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Structure-Activity Relationship
Substances
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Amides
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Benzimidazoles
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Indans
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MCHR1 protein, human
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Piperidines
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Receptors, Somatostatin