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

Moaz M. Abdou; Dewen Dong; Paul M. O'Neill; Eric Amigues; Magdalini Matziari

doi:10.1021/acsomega.2c03813

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

Moaz M. Abdou^*, Dewen Dong, Paul M. O'Neill, Eric Amigues, Magdalini Matziari

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

5 Citations (Scopus)

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 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.

Original language	English
Pages (from-to)	35035-35043
Number of pages	9
Journal	ACS Omega
Volume	7
Issue number	39
DOIs	https://doi.org/10.1021/acsomega.2c03813
Publication status	Published - 4 Oct 2022

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

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 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.",

author = "Abdou, \{Moaz M.\} and Dewen Dong and O'Neill, \{Paul M.\} and Eric Amigues and Magdalini Matziari",

note = "Funding Information: This work was financially supported by the Key Program Special Fund of XJTLU (KSF E-52). The authors express their appreciation and gratitude to Professor Edward D Sturrock, University of Cape Town, for doing the biological evaluation. Publisher Copyright: {\textcopyright} 2022 American Chemical Society. All rights reserved.",

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T1 - Design, Synthesis, and Study of a Novel RXPA380 - Proline Hybrid (RXPA380-P) as an Antihypertensive Agent

AU - Abdou, Moaz M.

AU - Dong, Dewen

AU - O'Neill, Paul M.

AU - Amigues, Eric

AU - Matziari, Magdalini

N1 - Funding Information: This work was financially supported by the Key Program Special Fund of XJTLU (KSF E-52). The authors express their appreciation and gratitude to Professor Edward D Sturrock, University of Cape Town, for doing the biological evaluation. Publisher Copyright: © 2022 American Chemical Society. All rights reserved.

PY - 2022/10/4

Y1 - 2022/10/4

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/85139566079

U2 - 10.1021/acsomega.2c03813

DO - 10.1021/acsomega.2c03813

M3 - Article

AN - SCOPUS:85139566079

VL - 7

SP - 35035

EP - 35043

JO - ACS Omega

JF - ACS Omega

IS - 39

ER -

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

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