The synthesis and Angiotensin Converting Enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives |
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| Authors: | Marco Bonesi Monica R Loizzo Giancarlo A Statti Sylvie Michel François Tillequin Francesco Menichini |
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| Institution: | 1. Department of Pharmaceutical Sciences, Faculty of Pharmacy, Nutrition and Health Sciences, University of Calabria, I-87030 Rende (CS), Italy;2. Laboratoire de Pharmacognosie de l’Université René Descartes, U.M.R./C.N.R.S. No. 8638, Faculté des Sciences Pharmaceutiques et Biologiques, 4, Avenue de l’Observatoire, F-75006 Paris, France |
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| 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). |
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