Phenoxyacetohydrazide schiff bases: β-glucuronidase inhibitors

• Published in: Molecules
• Main Author: Jamil W.; Perveen S.; Shah S.A.A.; Taha M.; Ismail N.H.; Perveen S.; Ambreen N.; Khan K.M.; Choudhary M.I.
• Format: Article
• Language: English
• Published: MDPI AG 2014
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-84904816945&doi=10.3390%2fmolecules19078788&partnerID=40&md5=4ea215c3b1b56d6b5540b58789414447
• ISSN: 14203049
• 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).