TY - JOUR
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 - http://www.scopus.com/inward/record.url?scp=85139566079&partnerID=8YFLogxK
U2 - 10.1021/acsomega.2c03813
DO - 10.1021/acsomega.2c03813
M3 - Article
AN - SCOPUS:85139566079
SN - 2470-1343
VL - 7
SP - 35035
EP - 35043
JO - ACS Omega
JF - ACS Omega
IS - 39
ER -