TY - JOUR
T1 - Synthesis of benzimidazole derivatives and their antiglycation, antioxidant, antiurease and molecular docking study
AU - Taha, Muhammad
AU - Rahim, Fazal
AU - Adalath, Bushra
AU - Imran, Syahrul
AU - Mohammed Khan, Khalid
AU - Adnan Ali shah, Syed
AU - Uddin, Nizam
AU - Nawaz, Muhammad
AU - Break, Mohammed Khaled Bin
AU - Magam, Sami M.
AU - Alqarni, Saad
N1 - Publisher Copyright:
© 2024 The Author(s)
PY - 2024/4
Y1 - 2024/4
N2 - Diabetes and ulcer are the major health problems all over the world. The present study reports synthesis and bio-evaluation of 19 benzimidazole analogs in search of antiglycation, antioxidant and antiulcer agents. The synthetic analogs were characterized using 1H NMR, 13C NMR and HR-EIMS. All compounds were checked for their antiglycation, antiurease and antioxidant activities. The fluorophenyl benzimidazole analogs 12–14 strongly inhibited glycation with IC50 values ranging from 142 µM to 193 µM. The same fluorophenyl analogs (12–14) were also found to exhibit the highest antioxidant activity with IC50 values ranging from 1.2 µM to 6.6 µM which further highlights the significance of these bioactive analogs. The dihydroxyphenyl analogs 6–9 demonstrated the most potent enzyme inhibitory activity with IC50 values ranging from 3.10 µM to 5.90 µM. Molecular docking studies were performed on the active analogs to investigate their interactions with the urease enzyme and provide a plausible explanation for their observed urease inhibitory activity.
AB - Diabetes and ulcer are the major health problems all over the world. The present study reports synthesis and bio-evaluation of 19 benzimidazole analogs in search of antiglycation, antioxidant and antiulcer agents. The synthetic analogs were characterized using 1H NMR, 13C NMR and HR-EIMS. All compounds were checked for their antiglycation, antiurease and antioxidant activities. The fluorophenyl benzimidazole analogs 12–14 strongly inhibited glycation with IC50 values ranging from 142 µM to 193 µM. The same fluorophenyl analogs (12–14) were also found to exhibit the highest antioxidant activity with IC50 values ranging from 1.2 µM to 6.6 µM which further highlights the significance of these bioactive analogs. The dihydroxyphenyl analogs 6–9 demonstrated the most potent enzyme inhibitory activity with IC50 values ranging from 3.10 µM to 5.90 µM. Molecular docking studies were performed on the active analogs to investigate their interactions with the urease enzyme and provide a plausible explanation for their observed urease inhibitory activity.
KW - Glycation
KW - In silico study
KW - Novel Benzimidazole derivatives
KW - Urease
UR - https://www.scopus.com/pages/publications/85186768002
U2 - 10.1016/j.arabjc.2024.105700
DO - 10.1016/j.arabjc.2024.105700
M3 - Article
AN - SCOPUS:85186768002
SN - 1878-5352
VL - 17
JO - Arabian Journal of Chemistry
JF - Arabian Journal of Chemistry
IS - 4
M1 - 105700
ER -