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Journal of enzyme inhibition and medicinal chemistry · 2020

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

СтатьяНазвание и аннотация: Перевод в очереди
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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

Аннотация

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.

Предметные рубрики MeSH

ИП Урсолов Владлен Сергеевич

ИНН 500118482352 · ОГРНИП 314500117700049

Реквизиты и контакты