Abstract
A new class of potent, orally active phenyl piperazine-based GH secretagogues have been discovered from attempts to mimic the arrangement of the phenyl substituent in the spiroindanyl piperidine and spiroindoline sulfonamide privileged structures of 4 and 1, respectively. The best of these compounds, 18 (EC50 = 2.8 nM) is nearly as potent as MK-0677 for releasing GH from rat pituitary cells.
MeSH terms
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Animals
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Cells, Cultured
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Drug Design
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Growth Hormone / metabolism*
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Indoles / pharmacology
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Molecular Mimicry
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Peptides / chemistry*
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Piperazines / chemical synthesis*
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Piperazines / pharmacology
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Pituitary Gland / cytology
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Pituitary Gland / drug effects
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Pituitary Gland / metabolism
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Rats
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Spiro Compounds / pharmacology
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Stimulation, Chemical
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / pharmacology
Substances
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1-(2-(2-amino-2-methylpropanamido)-5-phenylpentanoyl)-4-(4-(1-methylethylsulfonamido)phenyl)piperazine
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Indoles
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Peptides
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Piperazines
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Spiro Compounds
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Sulfonamides
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Growth Hormone
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ibutamoren mesylate