Phenoxyacetohydrazide Schiff Bases: β-Glucuronidase Inhibitors

Molecules

Waqas Jamil⁴  Shagufta Perveen⁴  Syed Adnan Ali Shah³  Muhammad Taha¹  Nor Hadiani Ismail¹  Shahnaz Perveen²  Nida Ambreen⁴  Khalid M. Khan⁴ 

[1] 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; E-Mails:;PCSIR Laboratories Complex, Shahrah-e-Dr. Salimuzzaman, Karachi 75280, Pakistan; E-Mail:;Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan 42300, Malaysia; E-Mail:;H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan; E-Mails:

关键词: phenoxyacetohydrazide;    Schiff bases;    β-glucouoronidase;    glucuronosyl-O-bonds;    D-saccharic acid-1;    4-lactone;   

DOI  :  10.3390/molecules19078788

来源: mdpi

【 摘 要 】

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).

【 授权许可】

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© 2014 by the authors; licensee MDPI, Basel, Switzerland.