| Title : Design, synthesis, and evaluation of novel bistrifluoromethyl-based hydrazones as dual inhibitors of acetylcholinesterase and carbonic anhydrase enzymes for Alzheimer's disease - Dincel_2024_Chem.Biol.Drug.Des_103_e14482 |
| Author(s) : Dincel ED , Basoglu-Unal F , Kuran ED , Kayra T , Aydin N , Kanber E , Gulcin I , Ulusoy-Guzeldemirci N |
| Ref : Chemical Biology Drug Des , 103 :e14482 , 2024 |
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Abstract :
In this project, non-sulfonamide bistrifluoromethyl-derived hydrazide-hydrazones were synthesized as multi-target-directed ligands to treat Alzheimer's disease and then, the novel derivatives were characterized by diverse spectral methods. Acetylcholinesterase (AChE), and human carbonic anhydrase (hCA) inhibitory qualifications of these compounds were determined. The reported compounds (2a-y) were determined to be effective inhibitors of the hCA I, hCA II and AChE enzymes with Ki values in the range of 1.130 +/- 0.15-5.440 +/- 0.93 microM for hCA I, 0.894 +/- 0.05-6.647 +/- 1.35 microM for hCA II, and 0.196 +/- 0.03-4.222 +/- 1.04 microM for AChE. In silico studies were also performed to illuminate the binding interactions. |
| PubMedSearch : Dincel_2024_Chem.Biol.Drug.Des_103_e14482 |
| PubMedID: 38378259 |
Dincel ED, Basoglu-Unal F, Kuran ED, Kayra T, Aydin N, Kanber E, Gulcin I, Ulusoy-Guzeldemirci N (2024)
Design, synthesis, and evaluation of novel bistrifluoromethyl-based hydrazones as dual inhibitors of acetylcholinesterase and carbonic anhydrase enzymes for Alzheimer's disease
Chemical Biology Drug Des
103 :e14482
Dincel ED, Basoglu-Unal F, Kuran ED, Kayra T, Aydin N, Kanber E, Gulcin I, Ulusoy-Guzeldemirci N (2024)
Chemical Biology Drug Des
103 :e14482