Publication: Influence of chirality of benzimidazole amine hybrids on inhibition of human erythrocytes carbonic anhydrase I, II and acetylcholinesterase
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2023-01-01
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Abstract
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.
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Biyomedikal Mühendisliği, Yaşam Bilimleri, Biyoteknoloji, Moleküler Biyoloji ve Genetik, Sitogenetik, Kimya, Temel Bilimler, Mühendislik ve Teknoloji, Biomedical Engineering, Life Sciences, Biotechnology, Molecular Biology and Genetics, Cytogenetic, Chemistry, Natural Sciences, Engineering and Technology, Mühendislik, Bilişim ve Teknoloji (ENG), Temel Bilimler (SCI), Yaşam Bilimleri (LIFE), Mühendislik, Mikrobiyoloji, BİYOKİMYA VE MOLEKÜLER BİYOLOJİ, BİYOTEKNOLOJİ VE UYGULAMALI MİKROBİYOLOJİ, MÜHENDİSLİK, BİYOMEDİKAL, Engineering, Computing & Technology (ENG), Natural Sciences (SCI), Life Sciences (LIFE), ENGINEERING, CHEMISTRY, MOLECULAR BIOLOGY & GENETICS, MICROBIOLOGY, BIOCHEMISTRY & MOLECULAR BIOLOGY, BIOTECHNOLOGY & APPLIED MICROBIOLOGY, ENGINEERING, BIOMEDICAL, Biyomühendislik, Fizik Bilimleri, Biyokimya, Genel Kimya, Moleküler Tıp, Moleküler Biyoloji, Bioengineering, Physical Sciences, Biochemistry, General Chemistry, Molecular Medicine, Molecular Biology, acetylcholinesterase, carbonic anhydrase, chiral benzimidazole, inhibition, molecular docking
Citation
Tunç T., ABDURRAHMANOĞLU S., Günel A., Alım Z., Demirel N., "Influence of Chirality of Benzimidazole Amine Hybrids on Inhibition of Human Erythrocytes Carbonic Anhydrase I, II and Acetylcholinesterase", Chemistry and Biodiversity, 2023