Design, synthesis, and evaluation of novel bistrifluoromethyl-based hydrazones as dual inhibitors of acetylcholinesterase and carbonic anhydrase enzymes for Alzheimer's disease

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Atıf İçin Kopyala

DİNCEL E. D., Başoğlu-Ünal F., Kuran E. D., Kayra T., Aydın N., Kanber E., ...Daha Fazla

Chemical Biology and Drug Design, cilt.103, sa.2, 2024 (SCI-Expanded)

• Yayın Türü: Makale / Tam Makale
• Cilt numarası: 103 Sayı: 2
• Basım Tarihi: 2024
• Doi Numarası: 10.1111/cbdd.14482
• Dergi Adı: Chemical Biology and Drug Design
• Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, BIOSIS, Biotechnology Research Abstracts, CAB Abstracts, Chemical Abstracts Core, EMBASE, MEDLINE, Veterinary Science Database
• Anahtar Kelimeler: acetylcholinesterase, carbonic anhydrase, hydrazide-hydrazone, molecular docking, synthesis
• İstanbul Üniversitesi Adresli: Evet

Özet

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.