Synthesis, In Vitro Anti-Microbial Analysis and Molecular Docking Study of Aliphatic Hydrazide-Based Benzene Sulphonamide Derivatives as Potent Inhibitors of α-Glucosidase and Urease

Shoaib Khan, Shahid Iqbal, Mazloom Shah, Wajid Rehman, Rafaqat Hussain, Liaqat Rasheed, Hamad Alrbyawi, Ayed A. Dera, Mohammed Issa Alahmdi, Rami Adel Pashameah, Eman Alzahrani, Abd Elaziem Farouk

Research output: Journal PublicationArticlepeer-review

18 Citations (Scopus)

Abstract

A unique series of sulphonamide derivatives was attempted to be synthesized in this study using a new and effective method. All of the synthesized compounds were verified using several spectroscopic methods, including FTIR, 1H-NMR, 13C-NMR, and HREI-MS, and their binding interactions were studied using molecular docking. The enzymes urease and α-glucosidase were evaluated against each derivative (1–15). When compared to their respective standard drug such as acarbose and thiourea, almost all compounds were shown to have excellent activity. Among the screened series, analogs 5 (IC50 = 3.20 ± 0.40 and 2.10 ± 0.10 µM) and 6 (IC50 = 2.50 ± 0.40 and 5.30 ± 0.20 µM), emerged as potent molecules when compared to the standard drugs acarbose (IC50 = 8.24 ± 0.08 µM) and urease (IC50 = 7.80 ± 0.30). Moreover, an anti-microbial study also demonstrated that analogs 5 and 6 were found with minimum inhibitory concentrations (MICs) in the presence of standard drugs streptomycin and terinafine.

Original languageEnglish
Article number7129
JournalMolecules
Volume27
Issue number20
DOIs
Publication statusPublished - Oct 2022
Externally publishedYes

Keywords

  • SAR and molecular docking
  • anti-microbial
  • anti-urease
  • sulphonamide
  • synthesis
  • α-glucosidase

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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