Synthesis, α-amylase inhibition and molecular docking study of bisindolylmethane sulfonamide derivatives

Muhammad Taha, Tayyaba Noreen, Syahrul Imran, Fasial Nawaz, Sridevi Chigurupati, Manikandan Selvaraj, Fazal Rahim, Nor Hadiani Ismail, Ashok Kumar, Ashik Mosaddik, Abdullah M. Alghamdi, Yousif Abdulrahman nasser alqahtani, Abdulaziz Abdulrahman nasser alqahtani

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16 Citations (Scopus)

Abstract

We have synthesized nineteen (1–19) bisindolylmethane sulfonamide analogs, characterized by different spectroscopic techniques such as 1HNMR and EI-MS and tested for α-amylase inhibitory potential. All compounds showed excellent to moderate degree of α-amylase inhibitory potential with IC50 values ranging between 1.192 ± 0.51 to 3.057 ± 0.18 μM as equated with standard acarbose (IC50 values 0.83 ± 0.36 μM). Among the series, six analogs such as 1, 4, 5, 6, 10, and 14 showed potent α-amylase inhibition with IC50 values 1.747 ± 0.2, 1.208 ± 0.15, 1.192 ± 0.51, 1.858 ± 0.08, 1.358 ± 0.27 and 1.527 ± 0.17 μM, respectively, as equated with standard acarbose. The structure-activity relationship based upon different substituents on phenyl part. Molecular docking studies performed to recognize the binding interaction of the most active compounds. [Figure not available: see fulltext.]

Original languageEnglish
Pages (from-to)2010-2022
Number of pages13
JournalMedicinal Chemistry Research
Volume28
Issue number11
DOIs
Publication statusPublished - Nov 2019

Keywords

  • Bisindolylmethane sulfonamide
  • Molecular docking
  • SAR
  • Synthesis
  • α-Amylase Inhibitory Potential

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