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Title: Iminopyrimidinones: A novel pharmacophore for the development of orally active renin inhibitors

Journal Article · · Bioorganic and Medicinal Chemistry Letters

The development of renin inhibitors with favorable oral pharmacokinetic profiles has been a longstanding challenge for the pharmaceutical industry. As part of our work to identify inhibitors of BACE1, we have previously developed iminopyrimidinones as a novel pharmacophore for aspartyl protease inhibition. In this letter we describe how we modified substitution around this pharmacophore to develop a potent, selective and orally active renin inhibitor.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
INDUSTRY
OSTI ID:
1404973
Journal Information:
Bioorganic and Medicinal Chemistry Letters, Vol. 25, Issue 7; ISSN 0960-894X
Publisher:
Elsevier
Country of Publication:
United States
Language:
ENGLISH