Chinese Journal of Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: May 20, 2025

Comprehensive Summary A unique type of natural coumarin skeleton‐based thiazolylbenzonitriles as novel structural scaffolds to exert potential multitargeting supramolecular antibacterial behavior was developed for the first time from resorcinol through multi‐step reactions. All new compounds were characterized by NMR and HRMS spectra. Structure‐activity relationships revealed that ethoxycarbonyl group optimal substituent effective action benzopyronyl (BTBs), BTB 13a gave an extremely low MIC value 0.002 mM against Staphylococcus aureus 29213, being 3‐fold more active than norfloxacin. Compound exerting most behaviour possessed favourable druggability with no obvious haemolysis, acceptable cytotoxicity propensity induce bacterial resistance. series medicinal chemobiological evaluations disclosed could not only intercalate into DNA produce stable biosupramolecular complexes block replication, form biosupermolecules gyrase, but also disturb cell membrane tempt leakage intracellular contents, fluctuate metabolism oxidative stress, finally resulting in death. Moreover, promising exhibited good vivo efficacy 29213. These results implied large promise members combat

Language: Английский