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Influence of Chirality of Benzimidazole Amine Hybrids on Inhibition of Human Erythrocytes Carbonic Anhydrase I, II and Acetylcholinesterase     
Yazarlar
Doç. Dr. Turgay TUNÇ Doç. Dr. Turgay TUNÇ
Kırşehir Ahi Evran Üniversitesi, Türkiye
Suzan Abdurrahmanoğlu
Marmara Üniversitesi, Türkiye
Prof. Dr. Aslıhan GÜNEL Prof. Dr. Aslıhan GÜNEL
Kırşehir Ahi Evran Üniversitesi, Türkiye
Doç. Dr. Zuhal ALIM Doç. Dr. Zuhal ALIM
Kırşehir Ahi Evran Üniversitesi, Türkiye
Prof. Dr. Nadir DEMİREL Prof. Dr. Nadir DEMİREL
Kırşehir Ahi Evran Üniversitesi, Türkiye
Özet
Novel chiral benzimidazole amine hybrids (4a–4d) were synthesized from commercially available amine [(R)- (+)-phenylethylamine, (−) (S)-(-)-phenylethylamine, (−) (R)-(-)-cyclohexylethylamine, (S)-(+)-cyclohexylethylamine] and 2-(chloromethyl)-N-tosyl-1H-benzimidazole. The synthesized compounds (4a–4d) were characterized by IR, NMR, and LC/MS analysis. The inhibitory effect of 4a–4d on human erythrocytes carbonic anhydrase I (hCA-I), II (hCA-II), and acetylcholinesterase (AChE) activity was investigated. For hCA-I, the IC50 values of 4a–4d were found to be 4.895 μM, 1.750 μM, 0.173 μM, and 0.620 μM, respectively, and for hCA-II, the IC50 values of 4a–4d were found to be 0.469 μM, 0.380 μM, 0.233 μM, 0.635 μM, respectively. Furthermore, IC50 values of 4a–4d on AChE were found as 87.5 nM, 100 nM, 26.92 nM, and 100 nM, respectively. In addition, molecular docking analysis was performed to evaluate the affinity of 4a–4d against hCA-I, hCA-II, and AChE and explain their binding interactions.
Anahtar Kelimeler
acetylcholinesterase | carbonic anhydrase | chiral benzimidazole | inhibition | molecular docking
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale
Dergi Adı Chemistry and Biodiversity
Dergi ISSN 1612-1872
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q3
Makale Dili İngilizce
Basım Tarihi 05-2023
Cilt No 20
Sayı 6
Sayfalar 1 / 9
Doi Numarası 10.1002/cbdv.202300207
Makale Linki http://dx.doi.org/10.1002/cbdv.202300207