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Design, Synthesis and Antibacterial Activity Evaluation of 4,5-Diphenyl-1<i>H</i>-Imidazoles Derivatives
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作者 Coulibaly Bamoro Fante Bamba +2 位作者 Koffi Téki Dindet Steve-Evanes Vallin Aurélie chagnault vincent 《Open Journal of Medicinal Chemistry》 CAS 2021年第2期17-26,共10页
<span style="font-family:Verdana;">Due to the continuous emergence and rapid spread of drug-resistant strains of bacteria, there is an urgent need for the development of novel antimicrobials. Along thi... <span style="font-family:Verdana;">Due to the continuous emergence and rapid spread of drug-resistant strains of bacteria, there is an urgent need for the development of novel antimicrobials. Along this line, the synthesis and antibacterial activity of 4,5-diphenylimidazol-2-thiol derivatives <strong>2a-g</strong> and <strong>6a-e</strong> are reported. The structures of the synthesized compounds were confirmed by Nuclear Magnetic Resonance (NMR) and High Resolution Mass Spectrometry (HRMS). All compounds were screened <em>in vitro</em> for their antibacterial activity against <em>Pseudomonas aeruginosa</em> and <em>Escherichia coli</em> (Gram-negative bacteria) and also against <em>Staphyloccocus aureus</em> and <em>Enterococcus faecalis</em> (Gram-positive bacteria). The results showed most of the synthesized compounds have no antibacterial activity. However compound <strong>6d</strong> was two-fold potent than ciprofloxacin against <em>Staphylococcus aureus</em> with Minimum Inhibitory Concentration (MIC) of 4 μg/mL and <strong>6c</strong> showed moderate biological activity against <em>Staphylococcus aureus</em> (16 μg/mL) and <em>Enterococcus faecalis</em> (16 μg/mL).</span> 展开更多
关键词 SYNTHESIS 4 5-diphenylimidazole-2-thiol BENZIMIDAZOLE Antibacterial Activity DRUG-RESISTANT
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