作者:Waqas Jamil、Shagufta Perveen、Syed Shah、Muhammad Taha、Nor Ismail、Shahnaz Perveen、Nida Ambreen、Khalid Khan、Muhammad Choudhary
DOI:10.3390/molecules19078788
日期:——
Phenoxyacetohydrazide Schiff base analogs 1–28 have been synthesized and their in vitro β-glucouoronidase inhibition potential studied. Compounds 1 (IC50 = 9.20 ± 0.32 µM), 5 (IC50 = 9.47 ± 0.16 µM), 7 (IC50 = 14.7 ± 0.19 µM), 8 (IC50 = 15.4 ± 1.56 µM), 11 (IC50 = 19.6 ± 0.62 µM), 12 (IC50 = 30.7 ± 1.49 µM), 15 (IC50 = 12.0 ± 0.16 µM), 21 (IC50 = 13.7 ± 0.40 µM) and 22 (IC50 = 22.0 ± 0.14 µM) showed promising β-glucuronidase inhibition activity, better than the standard (D-saccharic acid-1,4-lactone, IC50 = 48.4 ± 1.25 µM).
苯氧乙酰肼希夫碱类似物1-28已被合成,并研究了它们体外β-葡萄糖苷酸酶抑制潜力。化合物1(IC50 = 9.20 ± 0.32 µM)、5(IC50 = 9.47 ± 0.16 µM)、7(IC50 = 14.7 ± 0.19 µM)、8(IC50 = 15.4 ± 1.56 µM)、11(IC50 = 19.6 ± 0.62 µM)、12(IC50 = 30.7 ± 1.49 µM)、15(IC50 = 12.0 ± 0.16 µM)、21(IC50 = 13.7 ± 0.40 µM)和22(IC50 = 22.0 ± 0.14 µM)显示出有前景的β-葡萄糖苷酸酶抑制活性,优于标准品(D-糖酸-1,4-内酯,IC50 = 48.4 ± 1.25 µM)。