Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists.
A novel series of spirobenzazepines was synthesized and evaluated for V1a and V2 receptor antagonist activity. Compounds 8b, 8i, and 8k have shown selective V1a receptor antagonist activity. Compounds 8p and 8q were shown to be dual V1a/V2 receptor antagonists.
Xiang
Min Amy
MA
Endocrine Therapeutics and Metabolic Disorders, Johnson and Johnson Pharmaceutical Research and Development, L.L.C. 1000 Route 202, Bldg: PCC; Room: PC110, Raritan, NJ 08869-0602, USA.
Chen
Robert H
RH
Demarest
Keith T
KT
Gunnet
Joseph
J
Look
Richard
R
Hageman
William
W
Murray
William V
WV
Combs
Donald W
DW
Patel
Mona
M
D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines / Q000138:chemical synthesis / Q000494:pharmacology*; D002460:Cell Line; D000242:Cyclic AMP / Q000032:analysis; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D011485:Protein Binding; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines; D008024:Ligands; D013141:Spiro Compounds; D000242:Cyclic AMP