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

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 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.

SUBMITTER: Durgun M

PROVIDER: S-EPMC7170330 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

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

Durgun Mustafa M Türkeş Cüneyt C Işık Mesut M Demir Yeliz Y Saklı Ali A Kuru Ali A Güzel Abdussamat A Beydemir Şükrü Ş Akocak Suleyman S Osman Sameh M SM AlOthman Zeid Z Supuran Claudiu T CT

Journal of enzyme inhibition and medicinal chemistry 20201201 1

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 D ...[more]

PMID: 32249705

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

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Synthesis, characterisation, biological evaluation and <i>in silico</i> studies of sulphonamide Schiff bases.

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