Design, Synthesis, and Study of a Novel RXPA380–Proline Hybrid (RXPA380‑P) as an Antihypertensive Agent

In drug discovery, molecular modification over the lead molecule is often crucial for the development of a drug. Herein, we report the molecular hybridization design of a novel RXPA380–proline hybrid via linking the parent compound, phosphinic peptide RXPA380, with a proline analogue. The presented...

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Bibliographic Details
Published in:ACS omega 2022-10, Vol.7 (39), p.35035-35043
Main Authors: Abdou, Moaz M., Dong, Dewen, O’Neill, Paul M., Amigues, Eric, Matziari, Magdalini
Format: Article
Language:English
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Summary:In drug discovery, molecular modification over the lead molecule is often crucial for the development of a drug. Herein, we report the molecular hybridization design of a novel RXPA380–proline hybrid via linking the parent compound, phosphinic peptide RXPA380, with a proline analogue. The presented synthetic route is straightforward and produces the desired product RXPA380-P in moderate yield. The C- and N-domain constructs of the angiotensin-converting enzyme of RXPA380-P appeared to be poor inhibitors of ACE as compared to the parent compound RXPA380.
ISSN:2470-1343
2470-1343
DOI:10.1021/acsomega.2c03813