Renin inhibitors for the treatment of hypertension: Design and optimization of a novel series of pyridone-substituted piperidines

Article abstract of DOI:10.1016/j.bmcl.2011.05.013

An SAR campaign aimed at decreasing the overall lipophilicity of renin inhibitors such as 1 is described herein. It was found that replacement of the northern appendage in 1 with an N-methyl pyridone and subsequent re-optimization of the benzyl amide hand