Tetrazole based amides as growth hormone secretagogues.
A novel series of N1 substituted tetrazole amides were prepared and showed to be potent growth hormone (GH) secretagogues. Among them, hydroxyl containing analog 31 displayed 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 Research and Development, PO Box 5400, Princeton, NJ 08543-5400, USA. James.Li@bms.com
Wang
Haixia
H
Li
Jun
J
Qu
Fucheng
F
Swartz
Stephen G
SG
Hernández
Andrés S
AS
Biller
Scott A
SA
Robl
Jeffrey A
JA
Tino
Joseph A
JA
Slusarchyk
Dorothy
D
Seethala
Ramakrishna
R
Sleph
Paul
P
Yan
Mujing
M
Grover
Gary
G
Flynn
Neil
N
Murphy
Brian J
BJ
Gordon
David
D
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002460:Cell Line; D005910:Glioma / Q000378:metabolism; D013006:Growth Hormone / Q000097:blood / Q000378:metabolism*; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000737:chemistry*
D000577:Amides; D013777:Tetrazoles; C045574:1H-tetrazole; D013006:Growth Hormone