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European journal of medicinal chemistry v.143, 2018년, pp.1757 - 1767   SCI SCIE
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Synthesis of bis-indolylmethanes as new potential inhibitors of β-glucuronidase and their molecular docking studies

Taha, Muhammad (Department of clinical pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 31441, Dammam, Saudi Arabia ) ; Ullah, Hayat (Department of Chemistry, Hazara University, Mansehra 21300, Pakistan ) ; Al Muqarrabun, Laode Muhammad Ramadhan (Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300, Bandar Puncak Alam, Selangor, Malaysia ) ; Khan, Muhammad Naseem (Department of Chemistry, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan ) ; Rahim, Fazal (Department of Chemistry, Hazara University, Mansehra 21300, Pakistan ) ; Ahmat, Norizan (Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300, Bandar Puncak Alam, Selangor, Malaysia ) ; Ali, Muhammad (Department of Chemistry, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan ) ; Perveen, Shahnaz (PCSIR Laboratories Complex, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi 75280, Pakistan ) ;
  • 초록  

    Abstract Thirty-two (32) bis -indolylmethane-hydrazone hybrids 1 – 32 were synthesized and characterized by 1 HNMR, 13 CNNMR and HREI-MS. All compounds were evaluated in vitro for β -glucuronidase inhibitory potential. All analogs showed varying degree of β -glucuronidase inhibitory potential ranging from 0.10 ± 0.01 to 48.50 ± 1.10 μ M when compared with the standard drug D -saccharic acid-1,4-lactone (IC 50 value 48.30 ± 1.20 μ M). Derivatives 1–32 showed the highest β -glucuronidase inhibitory potentials which is many folds better than the standard drug D -saccharic acid-1,4-lactone. Further molecular docking study validated the experimental results. It was proposed that bis -indolylmethane may interact with some amino acid residues located within the active site of β -glucuronidase enzyme. This study has culminated in the identification of a new class of potent β -glucuronidase inhibitors. Highlights Synthesized of bis -indolylmethanes analogs. Evaluated in vitro β- glucuronidase activity. Identified a new c of β- glucuronidase inhibitors. Established Structure Activity Relationship. Performed Molecular docking. Graphical abstract [DISPLAY OMISSION]


  • 주제어

    Synthesis .   Bis-indolylmethanes .   β-Glucuronidase activity .   Molecular docking .   SAR.  

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