Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues.
Several novel series of tetrahydroisoquinoline 1-carboxamides were prepared and shown to be potent growth hormone (GH) secretagogues. Among them, carbamate 12a-E2 displays excellent in vivo activity by increasing plasma GH 10-fold in an anesthetized IV rat model.
Li
James J
JJ
Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA.
Wang
Haixia
H
Qu
Fucheng
F
Musial
Christa
C
Tino
Joseph A
JA
Robl
Jeffrey A
JA
Slusarchyk
Dorothy
D
Golla
Rajasree
R
Seethala
Ramakrishna
R
Dickinson
Kenneth
K
Giupponi
Leah
L
Grover
Gary
G
Sleph
Paul
P
Flynn
Neil
N
Murphy
Brian J
BJ
Gordon
David
D
Kung
Melissa
M
Stoffel
Robert
R
D000818:Animals; D013006:Growth Hormone / Q000097:blood / Q000378:metabolism*; D057927:Hydrophobic and Hydrophilic Interactions; D008956:Models, Chemical; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000097:blood / Q000378:metabolism*; D054440:Receptors, Ghrelin; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis / Q000494:pharmacology
D009842:Oligopeptides; D043562:Receptors, G-Protein-Coupled; D054440:Receptors, Ghrelin; D044005:Tetrahydroisoquinolines; C041048:growth hormone releasing hexapeptide; D013006:Growth Hormone