Preparation and biological evaluation of metronidazole derivatives with monoterpenes and eugenol

Chemical Biology & Drug Design
Majdi M BkhaitanHani S Faidah

Abstract

Two series of metronidazole derivatives (ester derivatives and ether derivatives) were prepared reacting metronidazole and its acetic acid oxidized form with menthol, thymol, carvacrol, and eugenol. Both series of compounds were tested in vitro against two strains of Helicobacter pylori (the ATCC 26695 and P12), and one strain of Clostridium (Clostridium perfringens). Most of the prepared compounds showed biological activity against the targeted bacteria. Compound 11 was highly active against all tested bacterial strains, especially against P12 with IC50 0.0011 μM/ml. Compound 6 was highly active against C. perfringens with MIC 0.0094 nM/ml. Viability test was conducted for compound 11 to test its selectivity for normal human fetal lung fibroblasts (MRC5), and it was found to be non-toxic with IC50 more than 50 μM/ml.

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Citations

May 29, 2019·Nucleosides, Nucleotides & Nucleic Acids·Agha Zeeshan Mirza
Nov 26, 2020·European Journal of Medicinal Chemistry·Om P S PatelRichard M Beteck
Feb 13, 2021·Evidence-based Complementary and Alternative Medicine : ECAM·Ammar BaderGhassan M Abushaikha
Apr 4, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Francesca SistoGabriella Mincione
Jul 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Maxim V MusalovSvetlana V Amosova

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