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

[Image: see text] 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 analog...

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Autores principales: Abdou, Moaz M., Dong, Dewen, O’Neill, Paul M., Amigues, Eric, Matziari, Magdalini
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9535653/
https://www.ncbi.nlm.nih.gov/pubmed/36211060
http://dx.doi.org/10.1021/acsomega.2c03813
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author Abdou, Moaz M.
Dong, Dewen
O’Neill, Paul M.
Amigues, Eric
Matziari, Magdalini
author_facet Abdou, Moaz M.
Dong, Dewen
O’Neill, Paul M.
Amigues, Eric
Matziari, Magdalini
author_sort Abdou, Moaz M.
collection PubMed
description [Image: see text] 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.
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spelling pubmed-95356532022-10-07 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. Amigues, Eric Matziari, Magdalini ACS Omega [Image: see text] 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. American Chemical Society 2022-09-23 /pmc/articles/PMC9535653/ /pubmed/36211060 http://dx.doi.org/10.1021/acsomega.2c03813 Text en © 2022 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Abdou, Moaz M.
Dong, Dewen
O’Neill, Paul M.
Amigues, Eric
Matziari, Magdalini
Design, Synthesis, and Study of a Novel RXPA380–Proline Hybrid (RXPA380-P) as an Antihypertensive Agent
title Design, Synthesis, and Study of a Novel RXPA380–Proline Hybrid (RXPA380-P) as an Antihypertensive Agent
title_full Design, Synthesis, and Study of a Novel RXPA380–Proline Hybrid (RXPA380-P) as an Antihypertensive Agent
title_fullStr Design, Synthesis, and Study of a Novel RXPA380–Proline Hybrid (RXPA380-P) as an Antihypertensive Agent
title_full_unstemmed Design, Synthesis, and Study of a Novel RXPA380–Proline Hybrid (RXPA380-P) as an Antihypertensive Agent
title_short Design, Synthesis, and Study of a Novel RXPA380–Proline Hybrid (RXPA380-P) as an Antihypertensive Agent
title_sort design, synthesis, and study of a novel rxpa380–proline hybrid (rxpa380-p) as an antihypertensive agent
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9535653/
https://www.ncbi.nlm.nih.gov/pubmed/36211060
http://dx.doi.org/10.1021/acsomega.2c03813
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