Acta Chim Slov. 2020 Dec;67(4):1139-1147.
1-Phenyl-5-substituted-3-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazole derivatives were synthesized from chalcone derivatives. The structures of compounds were characterized by IR, 1H NMR spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro antioxidant activity using DPPH and ABTS methods, anti-inflammatory activity using lipoxygenase inhibitory method and antidiabetic activity using the ?-glucosidase inhibitory method. Especially, pyrazoline derivatives exhibited stronger anti-inflammatory activity than the reference drug indomethacin (IC50: 50.45 µM) and their IC50 values were in the range of 0.68 and 4.45 µM. In addition, the ADME properties of all chalcone and pyrazoline derivatives were calculated by Lipinski's and Veber's rules.
1-苯基-5-取代-3-(4-(三氟甲基)苯基)-4,5-二氢-1H-吡唑衍生物由查尔酮衍生物合成得到。通过红外光谱、1H NMR 光谱方法和元素分析对化合物的结构进行了表征。采用 DPPH 和 ABTS 方法评估了所有化合物的体外抗氧化活性,采用脂氧合酶抑制法评估了抗炎活性,采用?-葡萄糖苷酶抑制法评估了抗糖尿病活性。特别是,吡唑啉衍生物表现出比参考药物吲哚美辛(IC50:50.45 μM)更强的抗炎活性,其 IC50 值在 0.68 和 4.45 μM 范围内。此外,通过 Lipinski 规则和 Veber 规则计算了所有查尔酮和吡唑啉衍生物的 ADME 性质。