苯氧乙酰肼席夫碱：β-葡萄糖醛酸酶抑制剂。
Phenoxyacetohydrazide Schiff bases: β-glucuronidase inhibitors.
作者信息
Jamil Waqas, Perveen Shagufta, Shah Syed Adnan Ali, Taha Muhammad, Ismail Nor Hadiani, Perveen Shahnaz, Ambreen Nida, Khan Khalid M, Choudhary Muhammad I
机构信息
Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan 42300, Malaysia.
出版信息
Molecules. 2014 Jun 25;19(7):8788-802. doi: 10.3390/molecules19078788.
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).
已合成苯氧乙酰肼席夫碱类似物1 - 28，并研究了它们在体外对β - 葡萄糖醛酸酶的抑制潜力。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）表现出有前景的β - 葡萄糖醛酸酶抑制活性，优于标准品（D - 糖二酸 - 1,4 - 内酯，IC50 = 48.4±1.25 μM）。
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