Design, Synthesis and Antibacterial Activity Evaluation of 4,5-Diphenyl-1<i>H</i>-Imidazoles Derivatives  

作　　者：Coulibaly Bamoro Fante Bamba Koffi Téki Dindet Steve-Evanes Vallin Aurélie Chagnault Vincent Coulibaly Bamoro;Fante Bamba;Koffi Téki Dindet Steve-Evanes;Vallin Aurélie;Chagnault Vincent(Laboratoire de Constitution et Réaction de la Matière, Université Félix Houphouët-Boigny, Abidjan, Cote d’Ivoire;Laboratoire de Glycochimie, des Antimicrobiens et des Agroressources (LG2A), UMR 7378 CNRS, Université de Picardie Jules Verne, Amiens, France)

机构地区：[1]Laboratoire de Constitution et Réaction de la Matière, Université Félix Houphouë t-Boigny, Abidjan, Cote d’Ivoire [2]Laboratoire de Glycochimie, des Antimicrobiens et des Agroressources (LG2A), UMR 7378 CNRS, Université de Picardie Jules Verne, Amiens, France

出　　处：《Open Journal of Medicinal Chemistry》2021年第2期17-26,共10页药物化学期刊（英文）

摘　　要：<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><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>

关 键 词：SYNTHESIS 4 5-diphenylimidazole-2-thiol BENZIMIDAZOLE Antibacterial Activity DRUG-RESISTANT 

分 类 号：O62[理学—有机化学]