The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives

Marco Bonesi; Monica R Loizzo; Giancarlo A Statti; Sylvie Michel; François Tillequin; Francesco Menichini

doi:10.1016/j.bmcl.2010.01.113

The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1990-3. doi: 10.1016/j.bmcl.2010.01.113. Epub 2010 Jan 25.

Authors

Marco Bonesi¹, Monica R Loizzo, Giancarlo A Statti, Sylvie Michel, François Tillequin, Francesco Menichini

Affiliation

¹ Department of Pharmaceutical Sciences, Faculty of Pharmacy, Nutrition and Health Sciences, University of Calabria, Rende (CS), Italy. bonesi@unical.it

PMID: 20167484
DOI: 10.1016/j.bmcl.2010.01.113

Abstract

A series of chalcones (1-9) and pyrazoles (10-18) was prepared to investigate their potential activity as Angiotensin I-Converting Enzyme (ACE) inhibitors. Their structures were verified by elemental analysis, UV, IR, MS, (1)H NMR, (13)C NMR, and 2D NMR experiments. Among tested compounds, chalcone 7 exerted the highest activity with an IC(50) value of 0.219 mM, while the most potent pyrazole was 15 (IC(50) value of 0.213 mM).

MeSH terms

Angiotensin-Converting Enzyme Inhibitors / chemical synthesis*
Angiotensin-Converting Enzyme Inhibitors / chemistry
Angiotensin-Converting Enzyme Inhibitors / pharmacology*
Chalcones / chemical synthesis*
Chalcones / chemistry
Chalcones / pharmacology*
Pyrazoles / chemistry*
Spectrum Analysis / methods

Substances

Angiotensin-Converting Enzyme Inhibitors
Chalcones
Pyrazoles