Synthesis, characterization and , biological evaluations of substituted benzimidazole derivatives.

A series of substituted benzimidazole derivatives were synthesized by reacting -phenylenediamine with various aromatic aldehydes or glycolic acid using various inexpensive reagents in aqueous media. Synthesized compounds were characterized and elucidated by IR, H NMR, ESI-MS spectra. Resultant compounds were screened for antimicrobial, cytotoxic, antioxidant, lipid peroxidation and cholinesterase inhibitory activities analgesic and anti-inflammatory, and anti-acetylcholinesterase and anti-butyrylcholinesterase activities. Among the synthesized compounds, compound showed most promising central analgesic effect (46.15%) compared to morphine (48.08%), whereas compounds , and showed significant peripheral analgesic activity at two different dose levels (25 mg/kg and 50 mg/kg). Compounds and at the dose of 100 mg/kg showed significant anti-inflammatory effects from the first hour and onward, whereas compounds and showed moderate cytotoxic activities. In addition, compound showed significant antioxidant activity having IC value of 16.73 µg/ml compared to 14.44 µg/ml for the standard BHT. Compound and exhibited mild to moderate cholinesterase inhibitory activity studies revealed that compound and might be suitable for cholinesterase inhibitory activity. A comprehensive computational and experimental data suggested compounds and as the best possible candidates for pharmacological activity. All the experimental data were statistically significant (p < 0.01 level).