Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists |
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| Authors: | Aimee L Crombie Thomas M Antrilli Brandon A Campbell David L Crandall Amedeo A Failli Yanan He Jeffrey C Kern William J Moore Lisa M Nogle Eugene J Trybulski |
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| Institution: | 1. Chemical Sciences, Pfizer Global Research and Development, 500 Arcola Road, Collegeville, PA 19335, USA;2. Cardiovascular and Metabolic Diseases Research, PGRD, 500 Arcola Road, Collegeville, PA 19335, USA;3. Discovery Analytical Chemistry, PGRD, 500 Arcola Road, Collegeville, PA 19335, USA;4. Chemical Sciences, PGRD, CN8000, Princeton, NJ 08543, USA |
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| Abstract: | 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 V1a/V2-receptor antagonist standard. |
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