Synthesis & Pharmacological Evaluation of Benzimidazole Derivatives

Abstract

Derivatives of Pyrimidine substituted benzimidazole were synthesized from chalcone derivatives of benzimidazole by condensation with guanidine hydrochloride. The synthesized compounds were confirmed by IR, 1H NMR and Mass spectral data. Synthesized derivatives were investigated for their anti-inflammatory, analgesic and antibacterial activities. Some of the synthesized compounds where found to possess significant anti-inflammatory, analgesic and antibacterial activities. The docking studies were carried out in 2OYE, 1CX2 and 1CQE receptors. It was found that SE-5B1 has 1CX2 receptor binding more than that of other receptors which is a clear indication that the molecule will have good anti-inflammatory activity with fewer side effects which was proved by anti inflammatory activity. Anti-inflammatory activity was carried out using carrageenan induced paw oedema method. The derivatives SE-5A1, SE-5A2, SE-5B1 and SE-5B2 showed moderate anti-inflammatory activity. Analgesic activity was carried out using hot plate method. The derivatives SE-5A4 and SE-5A5 showed good analgesic activity. Antibacterial was carried out using cup plate method at 75, 100, 125 μg/mL. Among all the synthesized compounds SE-5A1, SE-5A3, SE-5B3 and SE-5B5 showed good antibacterial activity. It was observed that the synthesized compounds possessing electron withdrawing (-NO2) in phenyl ring exhibited good pharmacological activities when compared to that of other synthesized compounds.