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Bioorg Med Chem Lett. 2010 Jun 15;20(12):3742-5. doi: 10.1016/j.bmcl.2010.04.068. Epub 2010 Apr 21.

Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists.

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1
Chemical Sciences, Pfizer Global Research and Development, Collegeville, PA 19335, USA. aimeecrombie@hotmail.com

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 V(1a)- and good V(2)-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)/V(2)-receptor antagonist standard.

PMID:
20471258
DOI:
10.1016/j.bmcl.2010.04.068
[Indexed for MEDLINE]

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