Skip to content
2000
Volume 14, Issue 2
  • ISSN: 2211-3525
  • E-ISSN: 2211-3533

Abstract

1,2,3-triazoles linked to bioactive alcohols of natural origin could have great pharmaceutical application as the literature reveals their antifungal, antibacterial, and anti-cancerous properties. These derivatives were synthesized using azide-alkyne cycloaddition strategy and subjected to evaluation for their antibacterial, antiplasmodial and anticancer properties. The drug likeliness was also evaluated by in silico physico-chemical prediction using QikProp version 3.2. The antimicrobial activities were evaluated against Plasmodium falciparum (P. falciparum), Escherichia coli (E. coli), Staphylococcus aureus (S. aureus) and Pseudomonas aeruginosa (P. aeruginosa) strains. The anti-cell proliferative activity was determined against four cancer cell lines (SK-MEL, KB, BT-546 and SK-OV-3). Five compounds (3a, 3c-f) showed antiplasmodial activity against chloroquin sensitive (D6) and chloroquin resistant (W2) strains of P. falciparum. Compound 3a (IC50 = 1.9 μg/mL) against P. falciparum D6 and 3c (IC50 = 2.7 μg/mL) against P. falciparum W2 strains were found as potential antiplasmodial agents. The antibacterial results against two gram negative (E. coli and P. aeruginosa) and one gram positive (S. aureus) strain also indicated the clinical potential of these compounds. Among all, compound 3c containing quinoline ring showed potent antibacterial property with IC50 values of 0.05, 6.23, and 7.4 μg/mL against P. aeruginosa, E. coli and S. aureus strains, respectively. Moreover, compound 3f derived from ferulic acid was found to exhibit promising anticancer activity against all the cancer cell lines used in the study.

Loading

Article metrics loading...

/content/journals/aia/10.2174/2211352514666160606115200
2016-08-01
2025-07-10
Loading full text...

Full text loading...

/content/journals/aia/10.2174/2211352514666160606115200
Loading

  • Article Type:
    Research Article
Keyword(s): 1; 2; 3-triazole; antibacterial; anticancer; antiplasmodial; physico-chemical properties
This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error
Please enter a valid_number test