Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives

Hyper-inflammation aggravates the symptoms of both communicable and non-communicable diseases. Therefore, anti-inflammatory compounds may have wide therapeutic application. Benzimidazole is a privileged scaffold and its success in drug development is evident from the long list of benzimidazole-based drugs with wide range of applications. This study was undertaken to develop new small molecules with anti-inflammatory properties. Compounds MBPHYD, MBNHYD and MBHYDX were synthesised, purified, characterised and found to be non-toxic both in vitro (in 100 μMconcentration for 24 h vs. 3000 Vero cells/well) and in vivo (at a dose of 100 mg/kg in female Wistar rats with animals observed for 48 h for any mortality). Compounds MBPHYD and MBNHYD were found to possess significant anti-inflammatory properties. Further, in silico analysis suggested their compliance with drug-likeness. While no toxicity was predicted, both compounds were suggested to have good oral bioavailability. Thus, results of this study may encourage further investigation to establish new anti-inflammatory benzimidazoles for application against various disease conditions.