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Synthesis and biological activities of phenyl piperazine-based peptidomimetic growth hormone secretagogues.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 1998 Jun 02; Vol. 8 (11), pp. 1431-6. - Publication Year :
- 1998
-
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.
- Subjects :
- Animals
Cells, Cultured
Drug Design
Indoles pharmacology
Molecular Mimicry
Piperazines pharmacology
Pituitary Gland cytology
Pituitary Gland drug effects
Pituitary Gland metabolism
Rats
Spiro Compounds pharmacology
Stimulation, Chemical
Structure-Activity Relationship
Sulfonamides pharmacology
Growth Hormone metabolism
Peptides chemistry
Piperazines chemical synthesis
Sulfonamides chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 8
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 9871779
- Full Text :
- https://doi.org/10.1016/s0960-894x(98)00238-8