The development of renin inhibitors with good oral PK has been a considerable  challenge for the industry over the past 25 years. As part of our work to identify  inhibitors of the aspartyl protease, BACE1, we developed novel cyclic acylguanidines that  interact with the catalytic aspartic acids in the active site. This talk will focus on  optimization of this pharmacophore for inhibition of renin  and the important role of  structure based drug design in the discovery of potent, selective and orally active renin  inhibitors.

Discovery of novel aspartyl protease inhibitors: The path from BACE to renin

243rd National Meeting (2012)

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