Potent 3-spiropiperidine growth hormone secretagogues

Systematic SAR studies of the different regioisomers and homologues of the spiro(indane-1,4′-piperidine) moiety in the growth hormone secretagogue L-162,752 are presented. Among them, spiro(3H-1-benzopyran-2,3′-piperidine) was found to afford secretagogues with low nanomolar in vitro activity. Syste...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-01, Vol.8 (1), p.107-112
Main Authors: Yang, Lihu, Morriello, Greg, Prendergast, Kristine, Cheng, Kang, Jacks, Tom, Chan, Wanda W.-S, Schleim, Klaus D, Smith, Roy G, Patchett, Arthur A
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Growth Hormone - metabolism
Hormones. Endocrine system
In Vitro Techniques
Indoles - chemistry
Indoles - pharmacology
Medical sciences
Pharmacology. Drug treatments
Piperidines - chemistry
Piperidines - pharmacology
Pituitary Gland - drug effects
Pituitary Gland - metabolism
Rats
Spiro Compounds - chemistry
Spiro Compounds - pharmacology
Structure-Activity Relationship
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Summary:Systematic SAR studies of the different regioisomers and homologues of the spiro(indane-1,4′-piperidine) moiety in the growth hormone secretagogue L-162,752 are presented. Among them, spiro(3H-1-benzopyran-2,3′-piperidine) was found to afford secretagogues with low nanomolar in vitro activity. Systematic SAR studies of the different regioisomers and homologues of the spiro(indane-1,4′-piperidine) moiety in the growth hormone secretagogue L-162,752 are presented. Among them, spiro(3H-1-benzopyran-2,3′-piperidine) was found to afford secretagogues with low nanomolar in vitro activity.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(97)10199-8