Novel Mannich bases derived from 1,2,4-triazoles: Design, synthesis, characterization, and glutathione S-transferase inhibition properties investigations
  
Yazarlar (9)
Doç. Dr. Onur AKYILDIRIM Kafkas Üniversitesi, Türkiye
Doç. Dr. Hilal MEDETALİBEYOĞLU Kafkas Üniversitesi, Türkiye
Ercan Oğuz Iğdır Üniversitesi, Türkiye
Abdülmelik Aras Iğdır Üniversitesi, Türkiye
Abdurrahman Atalay Karadeniz Technical University, Türkiye
Adem Korkmaz Muş Alparslan Üniversitesi, Türkiye
Doç. Dr. Murat BEYTUR Kafkas Üniversitesi, Türkiye
Fikret Türkan Iğdır Üniversitesi, Türkiye
Prof. Dr. Haydar YÜKSEK Kafkas Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı Journal of Molecular Structure (Q2)
Dergi ISSN 0022-2860 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili Türkçe Basım Tarihi 12-2023
Cilt / Sayı / Sayfa 1293 / 1 / 136321–136321 DOI 10.1016/j.molstruc.2023.136321
Makale Linki http://dx.doi.org/10.1016/j.molstruc.2023.136321
Özet
The reaction of variously substituted 1,2,4-triazole derivatives with morpholine and formaldehyde represents an efficient and easy-to-set synthetic entry toward heterocyclic N-Mannich bases. For this purpose, the synthesized Schiff Bases (3a-g) were reacted with formaldehyde and morpholine, a secondary amine, to yield novel N-Mannich bases (6a-g). The structures of the compounds (6a-g) were determined structurally by employing 1H/13C-NMR, IR, and elemental analysis. The synthesized compounds were screened for in vitro biological activity, and the bioanalysis results showed that the newly synthesized compounds had different in vitro enzyme inhibition activities against Glutathione S-transferase (GST). Their Ki values were calculated in the 2.69 ± 0.421–21.58±6.809 µM range. Besides, their IC50 values were calculated in the 1.975–2.753 µM range. Also, the potential inhibitory effects of the synthesized …
Anahtar Kelimeler
Enzyme inhibition | Glutathione S-transferase | Mannich bases | Molecular docking | Triazoles