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Phenoxyacetohydrazide Schiff bases: β-glucuronidase inhibitors

Jamil W 1 , Perveen S 2 , Shah SA 3 , Taha M 4 , Ismail NH 5 , Perveen S 6 Show all authors , Ambreen N 7 , Khan KM 8 , Choudhary MI 9

Affiliations 

  • 1 Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan. waqas143kh@yahoo.com
  • 2 Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan. sarosh.iqbal@yahoo.com
  • 3 Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan 42300, Malaysia. syedadnan@salam.uitm.edu.my
  • 4 Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Level 9, FF3, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan 42300, Malaysia. taha_hej@yahoo.com
  • 5 Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Level 9, FF3, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan 42300, Malaysia. norhadiani@puncakalam.uitm.edu.my
  • 6 PCSIR Laboratories Complex, Shahrah-e-Dr. Salimuzzaman, Karachi 75280, Pakistan. shamim_302@yahoo.com
  • 7 Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan. nida_mishi2002@yahoo.com
  • 8 Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan. khalid.khan@iccs.edu
  • 9 Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan. hassaan2@super.net.pk
Molecules, 2014 Jun 25;19(7):8788-802.
PMID: 24968334 DOI: 10.3390/molecules19078788

Abstract

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).

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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