New 1,2,3-triazole derivatives as acetylcholinesterase and carbonic anhydrase inhibitors: Synthesis, molecular docking, and solubility
Efeoglu, Cagla | Yabalak, Erdal | Nural, Yahya
In this study, a series of new 1,2,3-triazole derivatives were synthesized in 84-93 % yield using copper-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry and characterized by 1H/13C NMR, FT-IR, and HRMS analyses. The synthesized compounds (4a-h) were evaluated for their inhibitory activities against human carbonic anhydrase isoforms I and II (hCA I and hCA II) and acetylcholinesterase (AChE), which are clinically relevant targets in neurological and metabolic disorders. Among them, compounds 4f and 4g exhibited the most potent dual inhibitory activities. Compound 4f showed KI values of 144.30 nM for hCA II and 205.10 nM for AChE, while compound 4g exhibited KI values of 239.10 nM for hCA II and 125.90 nM for AChE. These values demonstrate that 4f and 4g are more effective than ...
Influence of Sublethal Chlorpyrifos Exposure on Oxıdative Stress and Acetylcholinesterase Activity in Common Carp (Cyprinus carpio)
YILMAZ, FERBAL ÖZKAN | HUNT, ARZU ÖZLÜER | YALIN, SERAP
The commonly used pesticides in agriculture cause enzyme inactivation and DNA damage via reacting with macromolecules and may also initiate peroxidation of poly-unsaturated fatty acids (PUFA) by generating of the reactive oxygen species (ROS), as a consequence they can lead to the oxidative stress. The objective of this study was to determine the oxidative and neurotoxic potential of sublethal chlorpyrifos in the brain tissue of Cyprinus carpio (C. carpio) for a period of 96 and 240 hours, respectively. Therefore, the levels of malondialdehyde (MDA), glutathione (GSH), advanced oxidation protein products (AOPP), protein carbonyl, and 8-hydroxydeoxyguanosine (8-OHdG) levels and activities of superoxide dismutase (SOD), catalase, glutathione peroxidase (GSH-Px) and acetylcholinesterase (AChE...