Phenoxyacetohydrazide Schiff Bases: β-Glucuronidase Inhibitors

Abstract

Phenoxyacetohydrazide Schiff base analogs 1-28 have been synthesized and their in vitro β-glucouoronidase inhibition potential studied. Compounds 1 (IC 50 = 9.20 ± 0.32 µM), 5 (IC 50 = 9.47 ± 0.16 µM), 7 (IC 50 = 14.7 ± 0.19 µM), 8 (IC 50 = 15.4 ± 1.56 µM), 11 (IC 50 = 19.6 ± 0.62 µM), 12 (IC 50 = 30.7 ± 1.49 µM), 15 (IC 50 = 12.0 ± 0.16 µM), 21 (IC 50 = 13.7 ± 0.40 µM) and 22 (IC 50 = 22.0 ± 0.14 µM) showed promising β-glucuronidase inhibition activity, better than the standard (D-saccharic acid-1,4-lactone, IC 50 = 48.4 ± 1.25 µM).

Therapeutic significance of β-glucuronidase activity and its inhibitors: A review

“…(IC 50 ¼ 1.60 mM) and 170 (IC 50 ¼ 2.20 mM) were the most active conjugates in the series. Similarly, phenoxyacetohydrazones [244] have displayed 2 to 5-fold improved potency compared to D-SAL (IC 50 ¼ 48.40 mM). Compounds 171 and 172 (Fig.…”

Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase

“…In a continued effort in search for biologically active molecules [20][21][22][23][24][25][26][27], here we are reporting synthesis of thiazole derivatives and their α-glucosidase inhibition activity not published earlier.…”

Novel 2,5-disubtituted-1,3,4-oxadiazoles with benzimidazole backbone: A new class of β-glucuronidase inhibitors and in silico studies

“…Elemental analyses were performed by using a Perkin-Elmer [48][49][50]. Furthermore to avoid precipitation, the concentration of the compounds was decreased and the reaction volume was high (200 micro liter) so the chance of precipitation was less hence the addition of detergents was not needed.…”