The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.
Synthesis and SAR of N-[4-[(4,5-dihydropyrazolo[3,4-d]thieno[3,2-b]azepin-6(2H)-y l)carbonyl]phenyl]benzamides as arginine vasopressin (AVP) receptor antagonists are discussed. Potent orally active AVP receptor antagonists are produced when the benzamide moiety contains a phenyl group at the 2-position. Similar analogues of 4,6,7,8-tetrahydro-5H-thieno[3,2-b]azepine and VPA-985 are reported.
Albright
J D
JD
Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY 10965, USA. albrigj@war.wyeth.com
Delos Santos
E G
EG
Dusza
J P
JP
Chan
P S
PS
Coupet
J
J
Ru
X
X
Mazandarani
H
H
D000818:Animals; D001127:Arginine Vasopressin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D001381:Azepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D017483:Receptors, Vasopressin / Q000378:metabolism; D013329:Structure-Activity Relationship
D001381:Azepines; D017483:Receptors, Vasopressin; D001127:Arginine Vasopressin