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Discovery of Novel 2-Carbamoyl Morpholine Derivatives as Highly Potent and Orally Active Direct Renin Inhibitors
- Source :
- ACS medicinal chemistry letters. 13(8)
- Publication Year :
- 2022
-
Abstract
- The renin-angiotensin-aldosterone system (RAAS) plays a key role in the regulation of blood pressure. Renin, the first and rate-limiting enzyme of the RAAS, is an attractive target for the treatment of hypertension and cardiovascular/renal diseases. Therefore, various direct renin inhibitors (DRIs) have been researched over recent decades; however, most exhibited poor pharmacokinetics and oral bioavailability due to the peptidomimetic or nonpeptidomimetic structures with a molecular weight (MW) of600, and only aliskiren is approved. This study introduces a novel class of DRIs comprised of a 2-carbamoyl morpholine scaffold. These compounds have a nonpeptidomimetic structure and a MW of500. The representative compound
- Subjects :
- Organic Chemistry
Drug Discovery
Biochemistry
Subjects
Details
- ISSN :
- 19485875
- Volume :
- 13
- Issue :
- 8
- Database :
- OpenAIRE
- Journal :
- ACS medicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....2a81141cb66d003b8b8e48a18c4a8af4