促酪氨酸酶抑制剂4-(5-(2,3-二氧基苯基)-3-(4-甲氧基苯基)-4,5-二氢- 1h -吡唑-1-y1)苯磺酰胺的合成

Rahayu Rahayu, Noval Herfindo, Nelly Oscifiani, N. Frimayanti, A. Zamri
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引用次数: 2

摘要

本研究以93%的产率成功合成了标题化合物5。吡唑啉化合物是由4-肼基苯磺酰胺3与查尔酮(E)-3-(2,3-二甲氧基苯基)-1-(4-甲氧基苯)丙-2-烯-1-酮4在碱性条件下的环缩合反应得到的。通过FTIR、NMR和HRMS光谱数据的分析,确定了其分子结构。此外,通过体外实验测定了其对双孢蘑菇酪氨酸酶的抑制活性。然而,吡唑啉化合物5显示出比阳性对照曲酸更低的抑制活性,而化合物5的IC50值高于曲酸。化合物5的IC50值为262.15µM,而曲酸的IC50为88.52µM。
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Synthesis of 4-(5-(2,3-Dimenthoxyphenyl)-3-(4-Methoxyphenyl)-4,5-Dihydro-1H-Pyrazol-1-y1) Benzenesulfonamide as a Promosing Tyrosinase Inhibitor Candidate
In this study, titled compound 5 has been successfully synthesized with 93% yield. The pyrazoline compound was obtained from the cyclocondensation reaction of 4-hydrazinylbenzenesulfonamide 3 with chalcone (E)-3-(2,3-dimethoxyphenyl)-1-(4-methoxyphenyl)prop-2-en-1-one 4 under basic conditions. The molecular structure was confirmed through analysis of FTIR, NMR and HRMS spectroscopic data. Furthermore, its tyrosinase enzyme inhibitory activity was determined through in vitro assay against tyrosinase of Agaricus bisporus. However, the pyrazoline compound 5 showed lower inhibitory activity than the positive control, kojic acid, whereas the IC50 value of the compound 5 is higher than that of kojic acid. The compound 5 IC50 value was 262.15 µM, while kojic acid IC50 value was 88.52 µM.
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