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)
Doç. Dr. Süleyman Akocak Adıyaman Üniversitesi, Türkiye
Doç. Dr. Nebih Lolak Adıyaman Üniversitesi, Türkiye
Doç. Dr. Hatice Esra DURAN Kafkas Üniversitesi, Türkiye
Prof. Dr. Mesut Işık Bilecik Şeyh Edebali Üniversitesi, Türkiye
Prof. Dr. Cüneyt Türkeş Erzincan Binali Yıldırım Üniversitesi, Türkiye
Prof. Dr. Mustafa Durgun Harran Üniversitesi, Türkiye
Prof. Dr. 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 Dergi Bilgileri (2023)
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili Türkçe Basım Tarihi 08-2023
Kabul Tarihi 20-07-2023 Yayınlanma Tarihi 01-08-2023
Cilt / Sayı / Sayfa 20 / 8 / – DOI 10.1002/cbdv.202300611
Makale Linki http://dx.doi.org/10.1002/cbdv.202300611
UAK Araştırma Alanları
Tıbbi Biyokimya
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 KI values in the range of 6.44±0.74‐86.85±7.01 nM for hCA I and with KI values in the range of 8.16±0.40‐77.29±9.56 nM for hCA II. Moreover, the new series of compounds …
Anahtar Kelimeler
1 | 3-diaryltriazene | carbonic anhydrase | glaucoma | molecular docking | sulfaguanidine