Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.
Small molecule agonists and antagonists of the V(2)-vasopressin receptor have been discovered and have undergone clinical trials. In conjunction with these discovery programs, the synthesis and biological testing of various metabolites associated with these clinical targets were actively pursued. We now report the results of our synthetic efforts and the corresponding biological data generated for several of the metabolites of WAY-151932 and CL-347985 (Lixivaptan).
Molinari
Albert J
AJ
Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. Molinaa@wyeth.com
Trybulski
Eugene J
EJ
Bagli
Jehan
J
Croce
Susan
S
Considine
John
J
Qi
Jian
J
Ali
Kadum
K
Demaio
William
W
Lihotz
Lynne
L
Cochran
David
D
D065092:Antidiuretic Hormone Receptor Antagonists; D001381:Azepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001552:Benzazepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D011758:Pyrroles; D017483:Receptors, Vasopressin / Q000819:agonists*; D001569:Benzodiazepines
D065092:Antidiuretic Hormone Receptor Antagonists; D001381:Azepines; D001549:Benzamides; D001552:Benzazepines; D011758:Pyrroles; D017483:Receptors, Vasopressin; C509746:WAY-151932; C409452:lixivaptan; D001569:Benzodiazepines