Yazarlar |
Doç. Dr. Turgay TUNÇ
Kırşehir Ahi Evran Üniversitesi, Türkiye |
Suzan Abdurrahmanoğlu
Türkiye |
Prof. Dr. Aslıhan GÜNEL
Türkiye |
Doç. Dr. Zuhal ALIM
Türkiye |
Prof. Dr. Nadir DEMİREL
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 mu M, 1.750 mu M, 0.173 mu M, and 0.620 mu M, respectively, and for hCA-II, the IC50 values of 4a-4d were found to be 0.469 mu M, 0.380 mu M, 0.233 mu M, 0.635 mu M, 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 & BIODIVERSITY |
Dergi ISSN | 1612-1872 |
Dergi Tarandığı Indeksler | SCI-Expanded |
Dergi Grubu | Q3 |
Makale Dili | Türkçe |
Basım Tarihi | 06-2023 |
Cilt No | 20 |
Sayı | 6 |
Doi Numarası | 10.1002/cbdv.202300207 |
Makale Linki | http://dx.doi.org/10.1002/cbdv.202300207 |