Bis-pyrimidine acetamides: design, synthesis and biological evaluation

Bis-pyrimidine acetamides: design, synthesis and biological evaluation Background: 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. 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. 1 13 Results: The synthesized bis-pyrimidine acetamide derivatives were confirmed by IR, H/ C-NMR, Mass spectral studies as well C, H, N analyses. The synthesized compounds were evaluated for their in vitro antimicrobial poten- tial 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 dilu- tion 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 (IC value) determined against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B (SRB) technique and 5-fluorouracil used as reference drug. Conclusions: The biological study demonstrated that compounds 3, 13, 16, 17 and 18 http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Chemistry Central Journal Springer Journals

Bis-pyrimidine acetamides: design, synthesis and biological evaluation

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Publisher
Springer International Publishing
Copyright
Copyright © 2017 by The Author(s)
Subject
Chemistry; Chemistry/Food Science, general
eISSN
1752-153X
D.O.I.
10.1186/s13065-017-0312-2
Publisher site
See Article on Publisher Site

Abstract

Background: 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. 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. 1 13 Results: The synthesized bis-pyrimidine acetamide derivatives were confirmed by IR, H/ C-NMR, Mass spectral studies as well C, H, N analyses. The synthesized compounds were evaluated for their in vitro antimicrobial poten- tial 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 dilu- tion 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 (IC value) determined against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B (SRB) technique and 5-fluorouracil used as reference drug. Conclusions: The biological study demonstrated that compounds 3, 13, 16, 17 and 18

Journal

Chemistry Central JournalSpringer Journals

Published: Aug 8, 2017

References

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