Novel Dibenzoazepine-Substituted Triazole Hybrids as Cholinesterase and Carbonic Anhydrase Inhibitors and Anticancer Agents: Synthesis, Characterization, Biological Evaluation, and In Silico Studies
Yazarlar (4)
Doç. Dr. Musa ERDOĞAN Kafkas Üniversitesi, Türkiye
Alper Önder
Çanakkale Onsekiz Mart Üniversitesi, Türkiye
Prof. Dr. Yeliz Demir Ardahan Üniversitesi, Türkiye
Dr. Öğr. Üyesi Ferah Cömert Önder Çanakkale Onsekiz Mart Üniversitesi, Türkiye
Makale Türü Açık Erişim Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı ACS Omega (Q2)
Dergi ISSN 2470-1343 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili Türkçe Basım Tarihi 11-2024
Cilt / Sayı / Sayfa 9 / 47 / 46860–46878 DOI 10.1021/acsomega.4c05804
Makale Linki http://dx.doi.org/10.1021/acsomega.4c05804
UAK Araştırma Alanları
Organik Kimya
Özet
The new dibenzoazepine-substituted triazole hybrids (12–20) were designed by molecular hybridization approach and synthesized utilizing the Cu(I)-catalyzed click reaction. The hybrid structures (12–20) were obtained in high yields (74–98%) with a simple two-step synthesis strategy and fully characterized. These compounds were assessed for their influence on various metabolic enzymes including human carbonic anhydrase isoenzymes (hCA I and hCA II), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). The Ki values for the compounds concerning hCA I, hCA II, AChE, and BChE enzymes were in the ranges 29.94–121.69, 17.72–89.42, 14.09–44.68, and 1.15–48.82 nM, respectively. Compound 13 was 49.70-fold more active than tacrine (standard drug) for BChE and 5.49-fold for AChE. Compound 14 was 4.16-fold more active than acetazolamide (standard drug) for hCA I and 5.79-fold for …
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