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|Title:||Synthesis and biological studies on 2 substituted benzimidazole derivatives|
|Keywords:||Synthesis and biological|
2-substituted benzimidazole derivatives
|Abstract:||Synthesis of N-(Benzimidazol-1-ylmethyl)-benzamide and N-(Benzimidazol- 1ylmethyl)-4-chlorobenzamide derivatives was done by Mannich reaction and evaluated for antimicrobial, antioxidant, anti-inflammatory, analgesic and ulcerogenic activity. The compounds were further characterized by spectral and analytical techniques. The synthesized compounds were screened for in vitro antimicrobial activity against gram positive, gram negative bacterial and fungal strains. Antioxidant activity of synthesized compounds was also checked by DPPH method using ascorbic acid as standard drug. Molecular docking studies of synthesized compounds were performed for antimicrobial and anti-inflammatory activity to study drug receptor interaction using docking program AutoDock Vina. From the in silico study among series-1 and series-2, 26 hit compounds with docking affinity higher than that of internal ligand SC-558 (-7.6 kcal/mol), were evaluated for anti-inflammatory and analgesic activity. On the basis of efficacy and potency of anti-inflammatory (p≤ 0.05) and analgesic (p≤ 0.01) potential, five compounds were selected each from series-1 and series-2 respectively for ulcerogenic activity. These compounds also showed significant (p≤ 0.05) results for ulcerogenic activity as compared to indomethacin as reference drug. Results revealed that molecules 3c, 3o and 3r from series-1 and 3a’, 3e’ and 3h’ from series-2 were most potent among all synthesized derivatives. Compounds were found to have good correlation with in-silico study.|
|Appears in Collections:||Doctoral Theses|
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