Abstract
The rising emergence of multidrug-resistant bacteria is becoming an increasingly serious threat to human health, therefore the development of structurally novel drugs has been an important topic worldwide to overcome drug-resistant strains. In this work, a series of novel acylhydrazone-bridged quinazolinone imidazoles were designed, synthesized and characterized by 1H NMR, 13C NMR and HRMS spectra. Bioactive assays showed that some target compounds exhibited significant antimicrobial potency. Especially, octadecyl derivative 6h and 4-fluorobenzyl derivative 7i showed 2.5 ~ 3.3 folds stronger activities against bacteria S. dysenteriae and E. coli DH52 than chloramphenicol, and 28 as well as 8.4 times higher efficacies toward fungus A. flavus than clinical drug fluconazole. The DNA-targeting preliminary exploration of highly active compound 7i by UV-Vis spectroscopy revealed that imidazole derivative 7i could intercalate into calf thymus DNA to form 7i -DNA supramolecular complex and thus block DNA replication to exert powerful antibacterial activities. Molecular docking study displayed that the active molecule 7i could form hydrogen bond with DNA base. This class of compounds as new type of specific anti- A. flavus and antibacterial drugs were worthy of being deeply investigated.
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