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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
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, (1)H-NMR, (13)C-NMR, and HREI-MS, and their binding interactions were studie...
Autores principales: | , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9609496/ https://www.ncbi.nlm.nih.gov/pubmed/36296720 http://dx.doi.org/10.3390/molecules27207129 |
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author | 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 |
author_facet | 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 |
author_sort | Khan, Shoaib |
collection | PubMed |
description | 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, (1)H-NMR, (13)C-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 (IC(50) = 3.20 ± 0.40 and 2.10 ± 0.10 µM) and 6 (IC(50) = 2.50 ± 0.40 and 5.30 ± 0.20 µM), emerged as potent molecules when compared to the standard drugs acarbose (IC(50) = 8.24 ± 0.08 µM) and urease (IC(50) = 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. |
format | Online Article Text |
id | pubmed-9609496 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-96094962022-10-28 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 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 Molecules Article 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, (1)H-NMR, (13)C-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 (IC(50) = 3.20 ± 0.40 and 2.10 ± 0.10 µM) and 6 (IC(50) = 2.50 ± 0.40 and 5.30 ± 0.20 µM), emerged as potent molecules when compared to the standard drugs acarbose (IC(50) = 8.24 ± 0.08 µM) and urease (IC(50) = 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. MDPI 2022-10-21 /pmc/articles/PMC9609496/ /pubmed/36296720 http://dx.doi.org/10.3390/molecules27207129 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article 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 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 |
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 |
title_full | 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 |
title_fullStr | 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 |
title_full_unstemmed | 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 |
title_short | 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 |
title_sort | 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 |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9609496/ https://www.ncbi.nlm.nih.gov/pubmed/36296720 http://dx.doi.org/10.3390/molecules27207129 |
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