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.
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Design, Synthesis, and Study of a Novel bRXPA380b-bProlineb Hybrid (bRXPA380-Pb) as an Antihypertensive Agent.pdf - Published version Download (2MB) | Preview |
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 |
|---|---|
| Divisions: | Faculty of Science and Engineering > School of Physical Sciences |
| Depositing User: | Symplectic Admin |
| Date Deposited: | 16 Feb 2023 17:29 |
| Last Modified: | 16 Feb 2023 17:29 |
| DOI: | 10.1021/acsomega.2c03813 |
| Related URLs: | |
| URI: | https://livrepository.liverpool.ac.uk/id/eprint/3168461 |
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