Zalaru Christina, Dumitrascu Florea, Draghici Constantin, Tarcomnicu Isabela, Marinescu Maria, Nitulescu George Mihai, Tatia Rodica, Moldovan Lucia, Popa Marcela, Chifiriuc Mariana Carmen
Department of Organic Chemistry, Biochemistry and Catalysis, Faculty of Chemistry, University of Bucharest, 90-92 Panduri Road, 030018 Bucharest, Romania.
"C.D. Nenitescu" Institute of Organic and Supramolecular Chemistry Romanian Academy, 202 B Spl. Independentei, 060023 Bucharest, Romania.
Antibiotics (Basel). 2022 Aug 12;11(8):1094. doi: 10.3390/antibiotics11081094.
A new series of pyrazolo-benzimidazole hybrid Mannich bases were synthesized, characterized by H-NMR, C-NMR, IR, UV-Vis, MS, and elemental analysis. In vitro cytotoxicity of the new compounds studied on fibroblast cells showed that the newly synthesized pyrazolo-benzimidazole hybrid derivatives were noncytotoxic until the concentration of 1 μM and two compounds presented a high degree of biocompatibility. The antibacterial and antibiofilm activity of the newly synthesized compounds was assayed on Gram-positive ATCC25923, ATCC29212, and Gram-negative ATCC27853, ATCC25922 strains. All synthesized compounds are more active against all three tested bacterial strains ATCC25923, ATCC29212, and ATCC25922 than reference drugs (Metronidazole, Nitrofurantoin), with the exception of compounds and , which are less active compared to Nitrofurantoin, and all synthesized compounds are more active against ATCC27853 compared to reference drugs (Metronidazole, Nitrofurantoin). Compound showed the best activity against ATCC 25923, with a MIC of 150 μg/mL and has also inhibited the biofilm formed by all the bacterial strains, having an MBIC of 310 µg/mL compared to the reference drugs (Metronidazole, Nitrofurantoin).
合成了一系列新的吡唑并苯并咪唑杂化曼尼希碱，通过氢核磁共振（H-NMR）、碳核磁共振（C-NMR）、红外光谱（IR）、紫外可见光谱（UV-Vis）、质谱（MS）和元素分析对其进行了表征。对新化合物在成纤维细胞上进行的体外细胞毒性研究表明，新合成的吡唑并苯并咪唑杂化衍生物在浓度达到1 μM时无细胞毒性，且有两种化合物表现出高度的生物相容性。对新合成化合物在革兰氏阳性菌ATCC25923、ATCC29212以及革兰氏阴性菌ATCC27853、ATCC25922菌株上测定了抗菌和抗生物膜活性。所有合成化合物对所有三种受试菌株ATCC25923、ATCC29212和ATCC25922的活性均高于参考药物（甲硝唑、呋喃妥因），但化合物 和 除外，它们与呋喃妥因相比活性较低，且所有合成化合物对ATCC27853的活性均高于参考药物（甲硝唑、呋喃妥因）。化合物 对ATCC 25923表现出最佳活性，最低抑菌浓度（MIC）为150 μg/mL，并且还抑制了所有细菌菌株形成的生物膜，与参考药物（甲硝唑、呋喃妥因）相比，其最低生物膜抑制浓度（MBIC）为310 µg/mL。
