Chemical biology & drug design · 2024
Design, synthesis, and evaluation of novel bistrifluoromethyl-based hydrazones as dual inhibitors of acetylcholinesterase and carbonic anhydrase enzymes for Alzheimer's disease.
СтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод в очереди
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Dincel Efe Doğukan, Başoğlu-Ünal Faika, Kuran Ebru Didem, Kayra Tülay, Aydın Nurcan, Kanber Esmanur, Gülçin İlhami, Ulusoy-Güzeldemirci Nuray
Аннотация
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 μM for hCA I, 0.894 ± 0.05-6.647 ± 1.35 μM for hCA II, and 0.196 ± 0.03-4.222 ± 1.04 μM for AChE. In silico studies were also performed to illuminate the binding interactions.