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Synthesis and Characterization of Novel 1,3‐Diaryltriazene‐Substituted Sulfaguanidine Derivatives as Selective Carbonic Anhydrase Inhibitors: Biological Evaluation, in Silico ADME/T and Molecular Docking Study      
Yazarlar
Süleyman Akocak
Adıyaman Üniversitesi, Türkiye
Nebih Lolak
Adıyaman Üniversitesi, Türkiye
Doç. Dr. Hatice Esra DURAN Doç. Dr. Hatice Esra DURAN
Kafkas Üniversitesi, Türkiye
Mesut Işık
Bilecik Şeyh Edebali Üniversitesi, Türkiye
Cüneyt Türkeş
Erzincan Binali Yıldırım Üniversitesi, Türkiye
Mustafa Durgun
Harran Üniversitesi, Türkiye
Şükrü Beydemir
Anadolu Üniversitesi, Türkiye
Özet
Sulfonamide compounds known as human carbonic anhydrase (hCA) inhibitors are used in the treatment of many diseases such as epilepsy, antibacterial, glaucoma, various diseases. 1,3-diaryl-substituted triazenes and sulfaguanidine are used for therapeutic purposes in many drug structures. Based on these two groups, the synthesis of new compounds is important. In the present study, the novel 1,3-diaryltriazene-substituted sulfaguanidine derivatives (SG1-13) were synthesized and fully characterized by spectroscopic and analytic methods. Inhibitory effect of these compounds on the hCA I and hCA II was screened as in vitro. All the series of synthesized compounds have been identified as potential hCA isoenzymes inhibitory with K values in the range of 6.44±0.74-86.85±7.01 nM for hCA I and with K values in the range of 8.16±0.40-77.29±9.56 nM for hCA II. Moreover, the new series of compounds showed a more effective inhibition effect than the acetazolamide used as a reference. The possible binding positions of the compounds with a binding affinity to the hCA I and hCA II was demonstrated by in silico studies. In conclusion, compounds with varying degrees of affinity for hCA isoenzymes have been designed and as selective hCA inhibitors. These compounds may be potential alternative agents that can be used to treat or prevent diseases associated with glaucoma and hCA inhibition.
Anahtar Kelimeler
1 | 3-diaryltriazene | carbonic anhydrase | glaucoma | molecular docking | sulfaguanidine
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale
Dergi Adı CHEMISTRY & BIODIVERSITY
Dergi ISSN 1612-1872
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q3
Makale Dili Türkçe
Basım Tarihi 08-2023
Cilt No 20
Sayı 8
Doi Numarası 10.1002/cbdv.202300611
Makale Linki http://dx.doi.org/10.1002/cbdv.202300611