Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 41, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.128030
Keywords
Isatin; Azoles; Antimicrobial; DNA
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Funding
- National Natural Science Foundation of China [21971212]
- Chongqing Special Foundation for Postdoctoral Research Proposal [Xm2016039]
- Program for Overseas Young Talents from State Administration of Foreign Experts Affairs, China [WQ2017XNDX047]
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The isatin hybridized 1,2,4-triazole 7a developed in this study exhibited excellent inhibitory activity against E. coli, possibly by blocking DNA replication.
Novel antibiotics are forced to be developed on account of multidrug-resistant bacteria with serious threats to human health. This work developed isatin-derived azoles as new potential antimicrobial agents. Bioactive assay revealed that isatin hybridized 1,2,4-triazole 7a exhibited excellent inhibitory activity against E. coli ATCC 25,922 with an MIC value of 1 ?g/mL, which was 8-fold more potent than reference drug norfloxacin. The active molecule 7a possessed the ability to kill some bacteria and fungi as well as displayed low propensity to induce resistance towards E. coli ATCC25922. Preliminary mechanism investigation indicated that hybrid 7a might block deoxyribonucleic acid (DNA) replication by intercalating with DNA and possibly interacting with DNA polymerase III, thus exerting its antimicrobial potency.
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