1238636-40-2Relevant academic research and scientific papers
Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists
Crombie, Aimee L.,Antrilli, Thomas M.,Campbell, Brandon A.,Crandall, David L.,Failli, Amedeo A.,He, Yanan,Kern, Jeffrey C.,Moore, William J.,Nogle, Lisa M.,Trybulski, Eugene J.
scheme or table, p. 3742 - 3745 (2010/08/22)
A series of biaryl amides containing an azabicyclooctane amine headpiece were synthesized and evaluated as mixed arginine vasopressin (AVP) receptor antagonists. Several analogues, including 8g, 12g, 13d, and 13g, were shown to have excellent V1a- and good V2-receptor binding affinities. Compound 13d was further profiled for drug-like properties and for an in vitro comparison with conivaptan, the program's mixed V 1a/V2-receptor antagonist standard.
