Abstract
BackgroundIn the past few years, increased resistance of microorganisms towards antimicrobial agents become a serious health problem, so there is a need for the discovery of new antimicrobial agents. On the other hand, bis-pyrimidines possess various types of biological activity. In view of this, in the present study we have designed and synthesized a new series of bis-pyrimidine acetamides by Claisen–Schmidt condensation and screened for its in vitro antimicrobial and anticancer activities.ResultsThe synthesized bis-pyrimidine acetamide derivatives were confirmed by IR, 1H/13C-NMR, Mass spectral studies as well C, H, N analyses. The synthesized compounds were evaluated for their in vitro antimicrobial potential against Gram positive (Staphylococcus aureus and Bacillus subtilis); Gram negative (Escherichia coli, Pseudomonas aeruginosa and Salmonella enterica) bacterial and fungal (Candida albicans and Aspergillus niger) strains by tube dilution technique and the minimum inhibitory concentration (MIC) recorded in µmol/mL was comparable to reference drugs, cefadroxil (antibacterial) and fluconazole (antifungal). The in vitro anticancer activity (IC50 value) determined against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B (SRB) technique and 5-fluorouracil used as reference drug.ConclusionsThe biological study demonstrated that compounds 3, 13, 16, 17 and 18 were found to be most active antimicrobial agents with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compounds 12, 16 and 18 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line with best IC50 value than the 5-fluorouracil (anticancer).Graphical abstractSAR of bis-pyrimidine acetamides
Highlights
In the past few years, increased resistance of microorganisms towards antimicrobial agents become a serious health problem, so there is a need for the discovery of new antimicrobial agents
Based on the literature survey and biological profile of bis-pyrimidine acetamides summarized in Fig. 2 and in continuation of our efforts in searching novel antimicrobial and anticancer agents [16–18], in the present work, we hereby report the synthesis, antimicrobial and anticancer activities of a series of bis-pyrimidine acetamide derivatives
Chemistry A general approach to synthesize the designed bispyrimidine acetamide derivatives based on Claisen– Schmidt condensation is outlined in Scheme 1
Summary
The biological study demonstrated that compounds 3, 13, 16, 17 and 18 were found to be most active antimicrobial agents with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compounds 12, 16 and 18 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line with best IC50 value than the 5-fluorouracil (anticancer).
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