Phenoxyacetohydrazide Schiff bases: β-glucuronidase inhibitors

Phenoxyacetohydrazide Schiff bases: β-glucuronidase inhibitors

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±...

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Veröffentlicht in:Molecules (Basel, Switzerland) Switzerland), 2014-06, Vol.19 (7), p.8788-8802
Hauptverfasser: Jamil, Waqas, Perveen, Shagufta, Shah, Syed Adnan Ali, Taha, Muhammad, Ismail, Nor Hadiani, Perveen, Shahnaz, Ambreen, Nida, Khan, Khalid M, Choudhary, Muhammad I
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Cattle
Enzyme Inhibitors - chemistry
Glucuronidase - antagonists & inhibitors
Glucuronidase - chemistry
glucuronosyl-O-bonds, D-saccharic acid-1,4-lactone
Hydrazines - chemistry
Phenoxyacetates - chemistry
phenoxyacetohydrazide
Schiff Bases
β-glucouoronidase
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Zusammenfassung: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).
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules19078788