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Biological Activities and In Silico Physico-Chemical Properties of 1,2,3- Triazoles Derived from Natural Bioactive Alcohols

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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.
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Keywords: 1; 2; 3-triazole; antibacterial; anticancer; antiplasmodial; physico-chemical properties

Document Type: Research Article

Publication date: August 1, 2016

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  • Anti-Infective Agents publishes original research, expert reviews, drug clinical trial studies and guest edited issues on all the latest and outstanding developments on the medicinal chemistry, biology, pharmacology and use of anti-infective and anti-parasitic agents. The scope of the journal covers all pre-clinical and clinical research on antimicrobials, antibacterials, antiviral, antifungal, and antiparasitic agents. Anti-Infective Agents is an essential journal for all infectious disease researchers in industry, academia and the health services.
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