Faculty of Arts and Sciences, Department of Chemistry, Recep Tayyip Erdogan University, Rize, Turkey.
Department of Chemistry and Chemical Processing Technology, Vocational School of Technical Studies, Recep Tayyip Erdogan University, Rize, Turkey.
Arch Pharm (Weinheim). 2018 Dec;351(12):e1800182. doi: 10.1002/ardp.201800182. Epub 2018 Oct 30.
A new series of quinazolinone hybrid molecules containing coumarin, furan, 1,2,4-triazole and 1,2,4-thiadiazole rings was designed, synthesized, and screened for their urease inhibition activities. All newly synthesized compounds showed outstanding urease inhibitory potentials with IC values ranging between 1.26 ± 0.07 and 7.35 ± 0.31 μg/mL. Among the series, coumarin derivatives (10a-d) exhibited the best inhibitory effect against urease in the range of IC = 1.26 ± 0.07 to 1.82 ± 0.10 μg/mL, when compared to standard urease inhibitors such as acetohydroxamic acid and thiourea (IC = 21.05 ± 0.96 and 15.08 ± 0.71 μg/mL, respectively). Molecular docking studies were also performed to analyze the binding mode of compound 10b, and supported the experimental results.
设计、合成了一系列新型的含香豆素、呋喃、1,2,4-三唑和 1,2,4-噻二唑环的喹唑啉酮杂合分子，并对其脲酶抑制活性进行了筛选。所有新合成的化合物均表现出优异的脲酶抑制潜力，IC 值范围在 1.26 ± 0.07 和 7.35 ± 0.31 μg/mL 之间。在这一系列中，香豆素衍生物（10a-d）在 1.26 ± 0.07 至 1.82 ± 0.10 μg/mL 的范围内对脲酶表现出最佳的抑制效果，与标准脲酶抑制剂如乙酰氧肟酸和硫脲（IC 分别为 21.05 ± 0.96 和 15.08 ± 0.71 μg/mL）相比。还进行了分子对接研究，以分析化合物 10b 的结合模式，实验结果得到了支持。
