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Synthesis of benzimidazole derivatives containing amide bond and biological evaluation as acetylcholinesterase, carbonic anhydrase I and II inhibitors     
Yazarlar
 Zuhal ALIM Zuhal ALIM
Kırşehir Ahi Evran Üniversitesi, Türkiye
 Turgay TUNÇ Turgay TUNÇ
Kırşehir Ahi Evran Üniversitesi, Türkiye
 Nadir DEMİREL Nadir DEMİREL
Kırşehir Ahi Evran Üniversitesi, Türkiye
 Aslıhan GÜNEL Aslıhan GÜNEL
Kırşehir Ahi Evran Üniversitesi, Türkiye
Nurcan Karacan
Gazi Üniversitesi, Türkiye
Özet
Acetylcholinesterase (AChE) and carbonic anhydrase I (CA-I) and II (CA-II) are two vital metabolic enzymes. AChE inhibitors are seen as target molecules in drug development studies for Alzheimer's treatment. CA inhibitors are target molecules for treating many diseases from glaucoma to cancer. For this reason, it is crucial to identify new AChE and CA inhibitors. In this study, four benzimidazole acetamide derivatives were synthesized and their inhibition effects were investigated against human erythrocyte carbonic anhydrase I (hCA-I), II (hCA-II), and AChE. IC50 values of 9a-10b were determined in the range of 0.936 to 17.07 µM for AChE. IC50 values of 9a–10b for hCA-I were found as 7.21 µM, 4.72 µM, 6.08 µM, 8.23 µM, respectively. On the other hand, IC50 values of 9a–9b for hCA-II were found as 8.64 µM, 7.07 µM, 4.12 µM, 5.93 µM, respectively. According to IC50 values, 9a–10b molecules exhibited strong inhibition effects for AChE and hCAI, II. Also, Molecular docking studies were carried out to explain the binding interaction of 9a–10b with AChE, hCA-I, and hCA-II.
Anahtar Kelimeler
Acetylcholinesterase | Benzimidazole | Carbonic anhydrase | Inhibition | Molecular docking
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale
Dergi Adı Elsevier BV
Dergi ISSN 0022-2860
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q3
Makale Dili İngilizce
Basım Tarihi 11-2022
Cilt No 1268
Sayı 133647
Doi Numarası 10.1016/j.molstruc.2022.133647
Makale Linki http://dx.doi.org/10.1016/j.molstruc.2022.133647