四取代咪唑类蘑菇酪氨酸酶抑制剂的一锅四组分合成、分子对接及药代动力学研究。

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Current pharmaceutical design Pub Date : 2025-01-02 DOI:10.2174/0113816128330769241113095033
Muhammad Naseem, Hummera Rafique, Sadia Roshan, Zaman Ashraf, Fouzia Perveen, Muhammad Tayyab
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引用次数: 0

摘要

介绍:在140°C下,将苯与芳香醛、酯取代胺和乙酸铵依次进行环缩合反应,回流近2小时,实现了四取代咪唑的高效四组分一锅简易合成。方法:每隔一段时间用薄层色谱法检测候补反应终点。采用物理数据对合成的1,2,4-四取代咪唑进行了表征,并用FTIR、NMR和元素分析等光谱技术对其结构特征进行了分析。结果:评价了制备的化合物对蘑菇基酪氨酸酶(多酚氧化酶)的抑制潜力。四取代咪唑衍生物具有显著的酪氨酸酶抑制活性。结论:进行了药动学机制及分子对接研究。
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One-pot, Four-component Synthesis, Molecular Docking and Pharmacokinetic Studies of Tetra-substituted Imidazole Derivatives as Potential Mushroom Tyrosinase Inhibitors.

Introduction: 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.

Method: 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.

Results: 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.

Conclusion: Pharmacokinetic mechanism and molecular docking studies were also carried out.

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来源期刊
CiteScore
6.30
自引率
0.00%
发文量
302
审稿时长
2 months
期刊介绍: Current Pharmaceutical Design publishes timely in-depth reviews and research articles from leading pharmaceutical researchers in the field, covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area guest edited by an acknowledged authority in the field. Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
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