Inhibitory Potential of a Novel Imidazole Derivative as Evaluated by Time-Kill and Dehydrogenase Activity
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Inhibitory Potential of a Novel Imidazole Derivative as Evaluated by Time-Kill and Dehydrogenase Activity Florin Aonofriesei • Simona Lupsor
Received: 21 July 2012 / Accepted: 1 October 2012 / Published online: 25 October 2012 Ó Springer Science+Business Media New York 2012
Abstract Antibacterial activity of 1,10 -methandiylbis(2methyl-1H-imidazole) (AIM) has been estimated both qualitatively and quantitatively against reference and clinical strains of Gram-positive and Gram-negative bacteria. MICs showed little variability among strains tested, ranging from 360 to 450 lg/ml and indicating rather a moderate antibacterial activity. Inhibition of dehydrogenase activity was significant in Escherichia coli ATCC 25922 and followed closely time-kill dynamics. Although moderate, AIM proved also to be useful on the ability to successfully inhibit the growth of antibiotic resistant clinical strains.
Introduction Imidazole moiety is well-known for its biological properties. Its derivatives are important therapeutic agents with a variety of applications: anticonvulsivant [1, 2], antihypertensive [3], antiviral [4, 5], antiprotozoaric [6] and antifungic [7, 8]. They have also good antibacterial effects and are active against a relatively wide range of bacteria [9–12]. Since imidazole moiety possess significant biological properties, we found interesting to evaluate the
F. Aonofriesei (&) Department of Biology–Ecology, Faculty of Natural Sciences and Agricultural Sciences, Ovidius University of Constanta, 1, University Street, 900470 Constanta, Romania e-mail: [email protected]
potential inhibitory activity of a new synthesized aminal of imidazole, 1,10 -methanediylbis(2-methyl-1N imidazole); (AIM) against Gram-positive and Gram-negative bacteria. Antibacterial activity of AIM was assessed both quantitatively and qualitatively using standard methods combined with evaluation of dehydrogenase activity (DHA).
Materials and Methods Chemistry The experimental data were previously published [12]. Synthesis was carried out by the condensation of paraformaldehyde (Riedel-de-Haen) with imidazole (Merck) by the single-mode Biotage Initiator 2.0. Reaction was conducted using tetrahydrofuran LiChrosolv (Merck) as solvent. The purity of AIM was established by high performance liquid chromatography (HPLC) performed on a CECIL CE4300 HPLC system equipped with UV–Vis (DAD) detector using MeOH : H2O (55 : 45) as eluent and a Varian Inertsil 5-ODS-2 column. The 1H-NMR spectra were recorded with Varian EM 360 Spectrometer using deuterio-chloroform (CDCl3) as solvent, and tetramethylsilane (TMS) as an internal standard. Mass spectra were obtained using Agilent 6400 Series Triple Quadrupole LC/MS equipped with electrospray ionization operated in positive ionization mode. Bacterial Strains
S. Lupsor Department of Chemistry and Chemical Engineering, Faculty of Physics, Chemistry, Electronics and Petroleum Chemistry, Ovidius University of Constanta, 124, Blvd. Mamaia, 900437 Constanta, Romania
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Activity of AIM was test
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