1303607-17-1Relevant articles and documents
The discovery and synthesis of potent zwitterionic inhibitors of renin
Aspiotis, Renee,Chen, Austin,Cauchon, Elizabeth,Dubé, Daniel,Falgueyret, Jean-Pierre,Gagné, Sébastien,Gallant, Michel,Grimm, Erich L.,Houle, Robert,Juteau, Hélne,Lacombe, Patrick,Laliberté, Sébastien,Lévesque, Jean-Franois,MacDonald, Dwight,McKay, Dan,Percival, M. David,Roy, Patrick,Soisson, Stephen M.,Wu, Tom
, p. 2430 - 2436 (2011/05/15)
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.