Yazarlar |
Doç. Dr. Turgay TUNÇ
Kırşehir Ahi Evran Üniversitesi, Türkiye |
Suzan Abdurrahmanoğlu
Marmara Üniversitesi, Türkiye |
Prof. Dr. Aslıhan GÜNEL
Kırşehir Ahi Evran Üniversitesi, Türkiye |
Doç. Dr. Zuhal ALIM
Kırşehir Ahi Evran Üniversitesi, Türkiye |
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 |