1310684-67-3Relevant academic research and scientific papers
Synthesis of benzimidazole based thiadiazole and carbohydrazide conjugates as glycogen synthase kinase-3β inhibitors with anti-depressant activity
Khan, Imran,Tantray, Mushtaq A.,Hamid, Hinna,Alam, Mohammad Sarwar,Kalam, Abul,Dhulap, Abhijeet
, p. 4020 - 4024 (2016/08/01)
A series of benzimidazole based thiadiazole and carbohydrazide conjugates have been synthesized and evaluated for inhibition of glycogen synthase kinase-3β and anti-depressant effect. Compounds 4f, 4j, 5b, 5g and 5i were found to be the most potent inhibitors of GSK-3β in vitro amongst the twenty-five benzimidazole based thiadiazole and carbohydrazide conjugates synthesized. Compound 5i was also found to exhibit significant antidepressant activity in vivo at 50?mg/kg, when compared to fluoxetine, a known antidepressant drug. The molecular docking studies revealed multiple hydrogen bond interactions by the synthesized compounds with various amino acid residues, viz, ASP-133, LYS-183, PRO-136, VAL-135, TYR-134, or LYS-60 at the GSK-3β receptor site.
Synthesis and biological activity of some triazole-bearing benzimidazole derivatives
Ansari,Lal,Khitoliya
, p. 341 - 352 (2012/01/05)
A number of N'-(arylmethylidene)-2-(2-methyl-1H-benzimidazol- -1-yl)acetohydrazide and 4-aryl-5-[(2-methyl-1H-benzimidazol-1-yl)methyl]- -4H-1,2,4-triazole-3-thiol derivatives were synthesized by incorporating various aromatic and heterocyclic substituents on 2-methyl-1H-benzimidazole. The structures of all the synthesized compounds were elucidated based on their elemental analyses and spectral data. The in vitro activities of these compounds against bacteria and fungi were evaluated by the disc diffusion and the minimum inhibitory concentration (MIC) methods. Some of the synthesized derivatives were found to be as active as kanamycin (standard drug).
