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- Title
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.
- Authors
Khan, Shoaib; Iqbal, Shahid; Shah, Mazloom; Rehman, Wajid; Hussain, Rafaqat; Rasheed, Liaqat; Alrbyawi, Hamad; Dera, Ayed A.; Alahmdi, Mohammed Issa; Pashameah, Rami Adel; Alzahrani, Eman; Farouk, Abd-ElAziem
- 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.
- Subjects
BENZENE derivatives; MOLECULAR docking; ANTI-infective agents; UREASE; DRUG standards; ALPHA-glucosidases; THIOUREA
- Publication
Molecules, 2022, Vol 27, Issue 20, p7129
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules27207129