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


Abdou, Moaz M, Dong, Dewen, O'Neill, Paul M ORCID: 0000-0003-4338-0317, Amigues, Eric and Matziari, Magdalini (2022) Design, Synthesis, and Study of a Novel RXPA380-Proline Hybrid (RXPA380-P) as an Antihypertensive Agent. ACS OMEGA, 7 (39). pp. 35035-35043. ISSN 2470-1343, 2470-1343

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Abstract

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 <b>RXPA380</b>-<b>proline</b> hybrid <i>via</i> linking the parent compound, phosphinic peptide <b>RXPA380</b>, with a proline analogue. The presented synthetic route is straightforward and produces the desired product <b>RXPA380-P</b> in moderate yield. The C- and N-domain constructs of the angiotensin-converting enzyme of <b>RXPA380-P</b> appeared to be poor inhibitors of ACE as compared to the parent compound <b>RXPA380</b>.

Item Type: Article
Uncontrolled Keywords: 3404 Medicinal and Biomolecular Chemistry, 34 Chemical Sciences, Biotechnology, 5.1 Pharmaceuticals
Divisions: Faculty of Science and Engineering > School of Physical Sciences
Depositing User: Symplectic Admin
Date Deposited: 16 Feb 2023 17:29
Last Modified: 12 Apr 2025 16:54
DOI: 10.1021/acsomega.2c03813
Related Websites:
URI: https://livrepository.liverpool.ac.uk/id/eprint/3168461
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