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 (7)
Süleyman Akocak Adıyaman Üniversitesi, Türkiye
Nebih Lolak Adıyaman Üniversitesi, Türkiye
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
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | CHEMISTRY & BIODIVERSITY (Q3) | ||
| Dergi ISSN | 1612-1872 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | Türkçe | Basım Tarihi | 08-2023 |
| Cilt / Sayı / Sayfa | 20 / 8 / – | DOI | 10.1002/cbdv.202300611 |
| Makale Linki | http://dx.doi.org/10.1002/cbdv.202300611 | ||
| 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 |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| WoS | 4 |
| Google Scholar | 6 |