Novel Naphthalimide Aminothiazoles as Potential Multitargeting Antimicrobial Agents.

ABSTRACT: A series of novel naphthalimide aminothiazoles were developed for the first time and evaluated for their antimicrobial activity. Some prepared compounds possessed good inhibitory activity against the tested bacteria and fungi. Noticeably, the piperazine derivative 4d displayed superior antibacterial activity against MRSA and Escherichia coli with MIC values of 4 and 8 μg/mL, respectively, to reference drugs. The most active compound 4d showed low toxicity against mammalian cells with no obvious triggering of the development of bacterial resistance, and it also possessed rapid bactericidal efficacy and efficient membrane permeability. Preliminarily investigations revealed that compound 4d could not only bind with gyrase-DNA complex through hydrogen bonds but coul

SUBMITTER: Chen YY 

PROVIDER: S-EPMC5733258 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature