The synthesis and Angiotensin Converting Enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives

doi:10.1016/j.bmcl.2010.01.113

Bioorganic & Medicinal Chemistry Letters

Volume 20, Issue 6, 15 March 2010, Pages 1990-1993

https://doi.org/10.1016/j.bmcl.2010.01.113 Get rights and content

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, ¹H NMR, ¹³C NMR, and 2D NMR experiments. Among tested compounds, chalcone 7 exerted the highest activity with an IC₅₀ value of 0.219 mM, while the most potent pyrazole was 15 (IC₅₀ value of 0.213 mM).

Graphical abstract

The synthesis and the ACE inhibitory activity of chalcones (1–9) and pyrazoles (10–18) are reported.

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Acknowledgments

The authors wish to thank Dr. Annamaria Caufin, Faculty of Pharmacy, Nutrition and Health Sciences, University of Calabria for revision of the English version of the manuscript.

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The synthesis and Angiotensin Converting Enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives

Abstract

Graphical abstract

Section snippets

Acknowledgments

Lancet

Lancet

Am. Heart J.

Am. J. Med.

Am. J. Clin. Nutr.

Cancer Lett.

FEBS Lett.

J. Ethnopharmacol.

Phytomedicine

Blood Press.

J. Clin. Hypertens.

Hypertension

Physiol. Rev.

Am. J. Nephrol.

Cardiovasc. Drug Ther.

Ann. Pharmacother.

Mini-Rev. Med. Chem.