Synthesis of novel derivatives of 4-methylbenzimidazole and evaluation of their biological activities

•We have synthesized novel derivatives of 4-methylbenzimidazole having benzoylhydrazide moiety 1–28.•Synthesized compound 1–28 were screened for antiglycation, antioxidant, antileishmanial and cytotoxicity activities.•Some of them showed potent antiglycation, antioxidant activity.•They (1–28) were non-toxic to the THP-1 cells.

4-Methylbenzimidazole 1–28 novel derivatives were synthesized and evaluated for their antiglycation and antioxidant activities. Compounds 1–7 and 11 showed excellent activities ranged 140–280 μM, better than standard drug rutin (294.46 ± 1.50 μM). Compound 1–28 were also evaluated for DPPH activities. Compounds 1–8 showed excellent activities, ranging 12–29 μM, better than standard drug n-propylgallate (IC50 = 30.30 ± 0.40 μM). For superoxide anion scavenging activity, compounds 1–7 showed better activity than standard n-propylgallate (IC50 = 106.34 ± 1.6 μM), ranged 82–104 μM. These compounds were found to be nontoxic to THP-1 cells.

Graphical abstractTwenty-eight (28) benzimidazole novel benzoylhydrazones were synthesized and evaluated their antiglycation, antioxidant, antileishmanial and cytotoxicity activities.Figure optionsDownload full-size imageDownload as PowerPoint slide