Click synthesis, antimicrobial, DNA photocleavage and computational studies of oxindole-tethered 1 H -1,2,3-triazoles.
Vijay KumarKashmiri LalRavinder KumarAnil KumarRamling S MathpatiMadhur Babu SinghKamlesh KumariPublished in: Future medicinal chemistry (2023)
Aim: To obtain new hybrids derived from isatin and triazole. Materials & methods: A series of oxindole-1- H -1,2,3-triazole hybrids ( 4a-l ) were synthesized from 3-sulfenylated N -propargylated oxindoles and organic azides employing Cu(I)-catalyzed azide-alkyne cycloaddition. These compounds were evaluated in vitro for antimicrobial activity by the standard serial dilution method and DNA photocleavage activity. Results: Antimicrobial assay revealed that compounds 4l and 4f exhibited promising efficacy against Candida albicans and Rhizopus oryzae , respectively, with a minimum inhibitory concentration (MIC) value of 0.0008 μmol/mL. Compounds 4h and 4k completely degraded plasmid DNA. Further molecular docking of compounds with 1KZN ( 4j and 4k ) and 5TZ1 ( 4h and 4l ) revealed good binding interactions. Conclusion: Results of the current research can help in the development of new antimicrobial agents with high efficacy.
Keyphrases
- molecular docking
- candida albicans
- circulating tumor
- staphylococcus aureus
- cell free
- single molecule
- biofilm formation
- escherichia coli
- single cell
- molecular dynamics simulations
- nucleic acid
- high throughput
- crispr cas
- room temperature
- circulating tumor cells
- high resolution
- cystic fibrosis
- liquid chromatography
- binding protein
- metal organic framework
- water soluble