2-(4-Fluorophenyl)-quinazolin-4(3H)-one (FQ) was synthesized, and its structure was identified with ¹H nuclear magnetic resonance (¹H NMR), ¹³C nuclear magnetic resonance (¹³C NMR), fourier transform infrared spectroscopy (FTIR), and high resolution mass spectrometry (HRMS). From the enzyme analysis, the results showed that it could inhibit the diphenolase activity of tyrosinase (IC₅₀ =120±2μM). Furthermore, the results of kinetic studies showed that the compound was a reversible mixed-type inhibitor, and that the inhibition constants were determined to be 703.2 (K _I) and 222.1μM (K _IS). The results of fluorescence quenching experiment showed that the compound could interact with tyrosinase and the substrates (tyrosine and l-DOPA). Molecular docking analysis revealed that the mass transfer rate was affected by FQ blocking the enzyme catalytic center. In brief, current study identified a novel tyrosinase inhibitor which deserved further study for hyperpigmentation drugs.

中文翻译：

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2-（4-氟苯基）-喹唑啉-4（3H）-一种新型酪氨酸酶抑制剂：合成，抑制活性和作用机理

合成了2-（4-氟苯基）-喹唑啉-4（3H）-一（FQ），并通过¹ H核磁共振（¹ H NMR），¹³ C核磁共振（¹³ C NMR）鉴定了其结构，傅立叶变换红外光谱（FTIR）和高分辨率质谱（HRMS）。通过酶分析，结果表明它可以抑制酪氨酸酶的双酚酶活性（IC ₅₀ = 120±2μM）。此外，动力学研究的结果表明该化合物是可逆的混合型抑制剂，其抑制常数确定为703.2（K _I）和222.1μM（K _IS）。荧光猝灭实验的结果表明该化合物可与酪氨酸酶和底物（酪氨酸和1-DOPA）相互作用。分子对接分析表明传质速率受FQ阻断酶催化中心的影响。简而言之，当前的研究确定了一种新型的酪氨酸酶抑制剂，值得对色素沉着过度的药物进行进一步的研究。