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Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases

Sulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, (13)C NMR, (1)H NMR, LC-MS and elemental analysis. Their inhibitory effect on AChE, and carbonic anhydrase I an...

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Autores principales: Durgun, Mustafa, Türkeş, Cüneyt, Işık, Mesut, Demir, Yeliz, Saklı, Ali, Kuru, Ali, Güzel, Abdussamat, Beydemir, Şükrü, Akocak, Suleyman, Osman, Sameh M., AlOthman, Zeid, Supuran, Claudiu T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7170330/
https://www.ncbi.nlm.nih.gov/pubmed/32249705
http://dx.doi.org/10.1080/14756366.2020.1746784
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author Durgun, Mustafa
Türkeş, Cüneyt
Işık, Mesut
Demir, Yeliz
Saklı, Ali
Kuru, Ali
Güzel, Abdussamat
Beydemir, Şükrü
Akocak, Suleyman
Osman, Sameh M.
AlOthman, Zeid
Supuran, Claudiu T.
author_facet Durgun, Mustafa
Türkeş, Cüneyt
Işık, Mesut
Demir, Yeliz
Saklı, Ali
Kuru, Ali
Güzel, Abdussamat
Beydemir, Şükrü
Akocak, Suleyman
Osman, Sameh M.
AlOthman, Zeid
Supuran, Claudiu T.
author_sort Durgun, Mustafa
collection PubMed
description Sulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, (13)C NMR, (1)H NMR, LC-MS and elemental analysis. Their inhibitory effect on AChE, and carbonic anhydrase I and II enzyme activities was investigated. Their antioxidant activity was determined using different bioanalytical assays such as radical scavenging tests with ABTS(•+), and DPPH(•+) as well as metal-reducing abilities with CUPRAC, and FRAP assays. All compounds showed satisfactory enzyme inhibitory potency in nanomolar concentrations against AChE and CA isoforms with K(I) values ranging from 10.14 ± 0.03 to 100.58 ± 1.90 nM. Amine group containing derivatives showed high metal reduction activity and about 70% ABTS radical scavenging activity. Due to their antioxidant activity and AChE inhibition, these novel compounds may be considered as leads for investigations in neurodegenerative diseases.
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spelling pubmed-71703302020-04-27 Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases Durgun, Mustafa Türkeş, Cüneyt Işık, Mesut Demir, Yeliz Saklı, Ali Kuru, Ali Güzel, Abdussamat Beydemir, Şükrü Akocak, Suleyman Osman, Sameh M. AlOthman, Zeid Supuran, Claudiu T. J Enzyme Inhib Med Chem Research Paper Sulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, (13)C NMR, (1)H NMR, LC-MS and elemental analysis. Their inhibitory effect on AChE, and carbonic anhydrase I and II enzyme activities was investigated. Their antioxidant activity was determined using different bioanalytical assays such as radical scavenging tests with ABTS(•+), and DPPH(•+) as well as metal-reducing abilities with CUPRAC, and FRAP assays. All compounds showed satisfactory enzyme inhibitory potency in nanomolar concentrations against AChE and CA isoforms with K(I) values ranging from 10.14 ± 0.03 to 100.58 ± 1.90 nM. Amine group containing derivatives showed high metal reduction activity and about 70% ABTS radical scavenging activity. Due to their antioxidant activity and AChE inhibition, these novel compounds may be considered as leads for investigations in neurodegenerative diseases. Taylor & Francis 2020-04-05 /pmc/articles/PMC7170330/ /pubmed/32249705 http://dx.doi.org/10.1080/14756366.2020.1746784 Text en © 2020 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Paper
Durgun, Mustafa
Türkeş, Cüneyt
Işık, Mesut
Demir, Yeliz
Saklı, Ali
Kuru, Ali
Güzel, Abdussamat
Beydemir, Şükrü
Akocak, Suleyman
Osman, Sameh M.
AlOthman, Zeid
Supuran, Claudiu T.
Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases
title Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases
title_full Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases
title_fullStr Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases
title_full_unstemmed Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases
title_short Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases
title_sort synthesis, characterisation, biological evaluation and in silico studies of sulphonamide schiff bases
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7170330/
https://www.ncbi.nlm.nih.gov/pubmed/32249705
http://dx.doi.org/10.1080/14756366.2020.1746784
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