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J Enzyme Inhib Med Chem ; 35(1): 950-962, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32249705

RESUMEN

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.


Asunto(s)
Antioxidantes/farmacología , Inhibidores de Anhidrasa Carbónica/farmacología , Inhibidores de la Colinesterasa/farmacología , Sulfonamidas/farmacología , Acetilcolinesterasa/metabolismo , Antioxidantes/síntesis química , Antioxidantes/química , Benzotiazoles/antagonistas & inhibidores , Inhibidores de Anhidrasa Carbónica/síntesis química , Inhibidores de Anhidrasa Carbónica/química , Anhidrasas Carbónicas/metabolismo , Inhibidores de la Colinesterasa/síntesis química , Inhibidores de la Colinesterasa/química , Relación Dosis-Respuesta a Droga , Humanos , Estructura Molecular , Bases de Schiff/síntesis química , Bases de Schiff/química , Bases de Schiff/farmacología , Relación Estructura-Actividad , Sulfonamidas/síntesis química , Sulfonamidas/química , Ácidos Sulfónicos/antagonistas & inhibidores
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