Abstract

Sulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, 13C NMR, 1H 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 KI 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.

Details

Title
Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases
Author
Durgun, Mustafa 1 ; Türkeş, Cüneyt 2 ; Işık, Mesut 3 ; Demir, Yeliz 4 ; Saklı, Ali 1   VIAFID ORCID Logo  ; Kuru, Ali 5 ; Güzel, Abdussamat 6 ; Beydemir, Şükrü 7 ; Akocak, Suleyman 8 ; Osman, Sameh M 9   VIAFID ORCID Logo  ; AlOthman, Zeid 9   VIAFID ORCID Logo  ; Supuran, Claudiu T 10 

1  Department of Chemistry, Faculty of Arts and Sciences, Harran University, Şanlıurfa, Turkey 
2  Department of Biochemistry, Faculty of Pharmacy, Erzincan Binali Yıldırım University, Erzincan, Turkey 
3  Department of Pharmacy Services, Vocational School of Health Services, Harran University, Şanlıurfa, Turkey 
4  Department of Pharmacy Services, Nihat Delibalta Göle Vocational High School, Ardahan University, Ardahan, Turkey 
5  Department of Chemistry, Faculty of Arts and Sciences, Harran University, Şanlıurfa, Turkey; Department of Chemistry, Faculty of Arts and Sciences, Sakarya University, Sakarya, Turkey 
6  Department of Pharmacy Services, Vocational School of Health Services, İnönü University, Malatya, Turkey 
7  Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey 
8  Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Adiyaman University, Adiyaman, Turkey 
9  Department of Chemistry, King Saud University, Riyadh, Kingdom of Saudi Arabia 
10  NEUROFARBA Department, Sezione di Scienze Farmaceutiche, Universita degli Studi di Firenze, Florence, Italy 
Pages
950-962
Publication year
2020
Publication date
Dec 2020
Publisher
Taylor & Francis Ltd.
ISSN
14756366
e-ISSN
14756374
Source type
Scholarly Journal
Language of publication
English
DOI
https://doi.org/10.1080/14756366.2020.1746784
ProQuest document ID
2463570901
Copyright
© 2020 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This work is licensed under the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.