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.
References
Jun 5, 2002·Toxicology Letters·Gisell Rodriguez FerreiroMarta Ana Carballo
May 27, 2005·Antimicrobial Agents and Chemotherapy·Domenico TrombettaGiuseppe Bisignano
Dec 24, 2005·Annals of Clinical Microbiology and Antimicrobials·Shaik Mahaboob AliNiyaz Ahmed
Dec 27, 2005·European Journal of Medicinal Chemistry·Franco ChimentiM Immacolata Brenciaglia
Mar 15, 2008·The Journal of Antimicrobial Chemotherapy·Boyan BonevJudicaël Parisot
Dec 17, 2008·Current Pharmaceutical Design·K Husnu Can Baser
Oct 7, 2009·Bioorganic & Medicinal Chemistry·Wen-Jun MaoHai-Liang Zhu
May 28, 2011·Scientia pharmaceutica·Rana M ObaidatAiman A Obaidat
Sep 18, 2012·European Journal of Medicinal Chemistry·Vivekkumar K Redasani, Sanjay B Bari
Oct 16, 2012·Mini Reviews in Medicinal Chemistry·Joseph A Farco, Oliver Grundmann
Apr 1, 2014·Bioorganic & Medicinal Chemistry·She-Feng WangHai-Liang Zhu
Jun 29, 2015·European Journal of Medicinal Chemistry·Angie M JarradMatthew A Cooper
Nov 26, 2015·Archives of Pharmacal Research·Faisal HayatDongyun Shin
Nov 26, 2015·Lancet·Alison H HolmesLaura J V Piddock
Dec 24, 2015·Alimentary Pharmacology & Therapeutics·I ThungM A Valasek
Apr 6, 2016·European Journal of Medicinal Chemistry·Beena NegiDiwan S Rawat
May 22, 2016·Chemical Biology & Drug Design·Long-Wang ChenHai-Liang Zhu
May 24, 2016·Food Chemistry·Anna MarcheseSeyed Mohammad Nabavi
Aug 16, 2016·Microbial Pathogenesis·Hanene MiladiKamel Chaieb
Jan 28, 2017·Journal of Molecular Graphics & Modelling·Svetlana JeremićZoran Marković
Apr 4, 2017·Chemical Biology & Drug Design·Majdi M BkhaitanAnna Piperno
Nov 21, 2017·Phytochemistry·Usama ShaheenAmmar Bader
Nov 24, 2017·Parasitology·David Leitsch
Dec 20, 2017·Oncology·Teppei AdachiMasatoshi Kudo
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