Naseem Muhammad, Rafique Hummera, Roshan Sadia, Ashraf Zaman, Perveen Fouzia, Tayyab Muhammad
Department of Chemistry, University of Gujrat, Gujrat 50700, Pakistan.
Department of Zoology, University of Gujrat, Gujrat 50700, Pakistan.
Curr Pharm Des. 2025;31(13):1078-1086. doi: 10.2174/0113816128330769241113095033.
An efficient and four-component one-pot facile synthesis of tetra-substituted imidazole is achieved by cyclo-condensation reaction of benzil with subsequent successive substitution of aromatic aldehydes, ester substituted amine and ammonium acetate via refluxing the mixture for almost two hours at 140°C.
The ending point of the understudy reaction was examined by TLC after regular intervals. Synthesized 1,2,4-tetrasubstituted imidazoles were characterized by physical data and the structural features were analyzed using spectroscopic techniques such as FTIR, NMR and elemental analysis.
The inhibition potential of fabricated compounds was evaluated against the mushroom based Tyrosinase (polyphenol oxidase) enzyme. Tetra-substituted imidazole derivatives demonstrated significant potent tyrosinase inhibition activities.
Pharmacokinetic mechanism and molecular docking studies were also carried out.
通过苯偶酰的环缩合反应，随后在140°C下将混合物回流近两小时，依次连续取代芳香醛、酯取代胺和乙酸铵，实现了高效的四组分一锅法简便合成四取代咪唑。
定期通过薄层色谱法（TLC）检测研究中反应的终点。合成的1,2,4-四取代咪唑通过物理数据进行表征，并使用傅里叶变换红外光谱（FTIR）、核磁共振（NMR）和元素分析等光谱技术分析其结构特征。
评估了所制备化合物对基于蘑菇的酪氨酸酶（多酚氧化酶）的抑制潜力。四取代咪唑衍生物表现出显著的酪氨酸酶抑制活性。
还进行了药代动力学机制和分子对接研究。
