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Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor
- Source :
- Journal of Medicinal Chemistry. 65:10882-10897
- Publication Year :
- 2022
- Publisher :
- American Chemical Society (ACS), 2022.
-
Abstract
- Renin is the rate-limiting enzyme in the renin-angiotensin-aldosterone system (RAAS) which regulates blood pressure and renal function and hence is an attractive target for the treatment of hypertension and cardiovascular/renal diseases. However, the development of direct renin inhibitors (DRIs) with favorable oral bioavailability has been a longstanding challenge for many years. This problem was thought to be because most of the reported DRIs were peptide-like structures or nonpeptide-like structures with a molecular weight (MW) of600. Therefore, we tried to find nonpeptidomimetic DRIs with a MW of500 and discovered the promising 2-carbamoyl morpholine derivative
Details
- ISSN :
- 15204804 and 00222623
- Volume :
- 65
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....7a7d118a6f7d7ab8858123b81a9c5444