| Literature DB >> 21429746 |
Renee Aspiotis1, Austin Chen, Elizabeth Cauchon, Daniel Dubé, Jean-Pierre Falgueyret, Sébastien Gagné, Michel Gallant, Erich L Grimm, Robert Houle, Hélène Juteau, Patrick Lacombe, Sébastien Laliberté, Jean-François Lévesque, Dwight MacDonald, Dan McKay, M David Percival, Patrick Roy, Stephen M Soisson, Tom Wu.
Abstract
The incorporation of a carboxylic acid within in a series of 3-amido-4-aryl substituted piperidines (represented by general structure 32) led to the discovery of potent, zwitterionic, renin inhibitors with improved off-target profiles (CYP3A4 time-dependent inhibition and hERG affinity) relative to analogous non-zwitterionic inhibitors of the past (i.e., 3). Strategies to address the oral absorption of these zwitterions are also discussed within.Entities:
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Year: 2011 PMID： 21429746 DOI： 10.1016/j.bmcl.2011.02.067
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823