Influence of Chirality of Benzimidazole Amine Hybrids on Inhibition of Human Erythrocytes Carbonic Anhydrase I, II and Acetylcholinesterase
Yazarlar (5)
Doç. Dr. Turgay TUNÇ
Kırşehir Ahi Evran Üniversitesi, Türkiye
Marmara Üniversitesi, Türkiye
Prof. Dr. Aslıhan GÜNEL
Kırşehir Ahi Evran Üniversitesi, Türkiye
Prof. Dr. Zuhal ALIM
Kırşehir Ahi Evran Üniversitesi, Türkiye
Prof. Dr. Nadir DEMİREL
Kırşehir Ahi Evran Üniversitesi, Türkiye
| Makale Türü |
Özgün Makale
(SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
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| Dergi Adı | Chemistry and Biodiversity (Q3) | ||
| Dergi ISSN | 1612-1872 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | Türkçe | Basım Tarihi | 06-2023 |
| Cilt / Sayı / Sayfa | 20 / 6 / – | DOI | 10.1002/cbdv.202300207 |
| Makale Linki | http://dx.doi.org/10.1002/cbdv.202300207 | ||
| 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 |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| SCOPUS | 3 |
| Google Scholar | 3 |