A library of nineteen new amide incorporated 1,2,3-triazole derivatives have been
synthesized and evaluated for antioxidant and antimicrobial activities. Firstly, 1,2,3-triazole
derivative, (2-[{1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl}methoxy]benzoic acid) 4 was
prepared by click chemistry using methyl salicylate 1 as starting material. This key
intermediate 4 was coupled with different aromatic amines, aliphatic amines and acid
hydrazide using HoBt and EDC as coupling agent to get the amide incorporated 1,2,3-triazole
derivatives as target compounds 5-23. All the new compounds were evaluated for antioxidant
and antimicrobial activities. The antioxidant activity was performed by DPPH assay. The
antimicrobial activity was done by disc diffusion method against bacterial and fungal strains.
Further MIC was calculated for six compounds (6, 9, 10, 18, 19 and 22) against two gram
positive (S.aureus, E.faecalis) and two gram negative (E.coli, P.aerugenosa) bacterial strains.
Among the tested compounds, two compounds 6 and 19 showed superior DPPH scavenging
activity with 94.12 and 95.64% inhibition, respectively compared to the standard molecule
ascorbic acid which showed 91.80% inhibition. Compounds 6 and 19 revealed strong
antimicrobial effect. Compound 6 showed MIC 25 ?g/disk against E. coli and E.faecalis,
compared to the standard drug Amoxicillin which showed MIC 12.5 and >25 ?g/disk
respectively. Compound 19 showed MIC 25 ?g/disk against E. coli and 50 ?g/disk against
P.aerugenosa compared to standard drug Amoxicillin which showed MIC 12.5 and 25 ?g/disk, respectively. From the antioxidant and antimicrobial results, it can be concluded that
compounds 6 and 19 may be used as a lead molecule in the development of more potent
antibacterial agent in future.
Keywords: Amide incorporated 1,2,3-Triazole, Click Chemistry, Antioxidant, Antibacterial,
Antifungal; Minimum inhibitory concentration
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https://doi.org/10.31032/IJBPAS/2019/8.4.4690
