Abstract
BackgroundA series of benzimidazole derivatives was developed and its chemical scaffolds were authenticated by NMR, IR, elemental analyses and physicochemical properties. The synthesized compounds were screened for their antimicrobial and antiproliferative activities.Results and discussionThe synthesized benzimidazole compounds were evaluated for their antimicrobial activity using the tube dilution method and were found to exhibit good antimicrobial potential against selected Gram negative and positive bacterial and fungal species. The compounds were also assessed for their anticancer activity exhibited using the SRB assay and were found to elicit antiproliferative activity against MCF7 breast cancer cell line, which was comparable to the standard drug.ConclusionAntimicrobial screening results indicated that compounds 1, 2 and 19 to be promising antimicrobial agents against selected microbial species and comparable to standard drugs which included norfloxacin and fluconazole. The anticancer screening results revealed that compounds, 12, 21, 22 and 29 to show the highest activity against MCF7 and their IC50 values were more potent than 5-fluorouracil.
Highlights
A series of benzimidazole derivatives was developed and its chemical scaffolds were authenticated by NMR, IR, elemental analyses and physicochemical properties
Antimicrobial screening results indicated that compounds 1, 2 and 19 to be promising antimicrobial agents against selected microbial species and comparable to standard drugs which included norfloxacin and fluconazole
The anticancer screening results revealed that compounds, 12, 21, 22 and 29 to show the highest activity against MCF7 and their IC50 values were more potent than 5-fluorouracil
Summary
Chemistry Target compounds (1–30) were synthesized by following procedure outlined in Scheme 1. It has been noticed that the antibacterial activity of Schiff bases against E. coli enhanced due to the presence of vinyl group between benzimidazole amine and N-benzylidene moiety and the substitution of electron releasing group at phenyl nucleus as in the compound 1 and the same moiety improved anticancer activity of methanone derivatives as in compound 22. The electron donating group placed at phenyl ring attached to N-alylidene/arylidene moiety along with presence of electron withdrawing group on phenyl ring attached to methanone moiety improved antibacterial and antifungal activity of synthesized benzimidazole derivatives against bacterial and fungal strains as in compound 19. Anticancer screening results (Table 2) indicated that compound 22 (IC50 = 0.9 μM) was found to be the most potent when compared to the standard drug, 5-fluorouracil (IC50 = 35.4 μM).
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