Potent 3-spiropiperidine growth hormone secretagogues

• Published in: Bioorganic & medicinal chemistry letters Vol. 8; no. 1; pp. 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: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 06-01-1998; Elsevier
• 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; Rat; Nitrogen heterocycle; Rodentia; Oxygen heterocycle; In vitro; Spiran; Vertebrata; Mammalia; Structure activity relation; Animal; Six membered ring; Piperidine derivatives; Bicyclic compound; Carboxamide; Aromatic compound; Hormone releasing factor; Indole derivatives; Chemical synthesis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(97)10199-8

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.