Abstract
BackgroundA new series of benzoxazole analogues was synthesized and checked for their in vitro antibacterial, antifungal and anticancer activities.Results and discussionThe synthesized benzoxazole compounds were confirmed by IR, 1H/13C-NMR, mass and screened for their in vitro antimicrobial activity against Gram-positive bacterium: Bacillus subtilis, four Gram-negative bacteria: Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi and two fungal strains: Candida albicans and Aspergillus niger using tube dilution technique and minimum inhibitory concentration (MIC) was noted in µM and compared to ofloxacin and fluconazole. Human colorectal carcinoma (HCT116) cancer cell line was used for the determination of in vitro anticancer activity (IC50 value) by Sulforhodamine B assay using 5-fluorouracil as standard drug.ConclusionThe performed study indicated that the compounds 1, 10, 13, 16, 19, 20 and 24 had highest antimicrobial activity with MIC values comparable to ofloxacin and fluconazole and compounds 4, 6, 25 and 26 had best anticancer activity in comparison to 5-fluorouracil.
Highlights
A new series of benzoxazole analogues was synthesized and checked for their in vitro antibacterial, antifungal and anticancer activities
Chemistry The method to synthesize the designed benzoxazole derivatives is given in Scheme 1
The results indicated that the compound 6 (IC50 = 24.5 μM) exhibited the best anticancer activity in comparison with the standard drug (IC50 = 29.2 μM) whereas the compounds 4 and 26 displayed IC50 values closer to the reference drug (39.9 μM and 35.6 μM, respectively)
Summary
A series of new benzoxazole derivatives was prepared and its chemical structure was confirmed by 1H/13C NMR, Mass and IR studies. All the derivatives were further evaluated for antibacterial, antifungal and anticancer activity and it was observed that the compounds 1, 10, 13, 16, 19, 20 and 24 displayed the best activity against various microbial species in comparison to reference drug ofloxacin and fluconazole. Authors’ contributions The designing, synthesis, antimicrobial activity and spectral analysis of the prepared benzoxazole derivatives was done by the authors BN, SK and ST. 2 Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia. 3 Collaborative Drug Discovery Research (CDDR) Group, Pharmaceutical Life Sciences Community of Research, Universiti Teknologi MARA (UiTM), 40450 Shah Alam, Selangor Darul Ehsan, Malaysia. 5 Atta‐ur‐Rahman Institute for Natural Products Discovery (AuRIns), Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia
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