In this paper, synthesis and antimicrobial studies of 31 novel coumarin-substituted pyrazole derivatives are reported. Some of these compounds have shown potent activity against methicillin-resistant Staphylococcus aureus (MRSA) with minimum inhibitory concentration (MIC) as low as 3.125 µg/mL. These molecules are equally potent at inhibiting the development of MRSA biofilm and the destruction of preformed biofilm. These results are very significant as MRSA strains have emerged as one of the most menacing pathogens of humans and this bacterium is bypassing HIV in terms of fatality rate.
We report the synthesis and antimicrobial studies of a new series of naphthyl-substituted pyrazole-derived hydrazones. Many of these novel compounds are potent growth inhibitors of several strains of drug-resistant bacteria. These potent compounds have inclined growth inhibitory properties for planktonic
Staphylococcus aureus
and
Acinetobacter baumannii,
and its drug-resistant variants with minimum inhibitory concentration (MIC) as low as 0.78 and 1.56 μg/mL respectively. These compounds also show potent activity against
S. aureus
and
A. baumannii
biofilm formation and eradication properties. Time Kill Assay shows that these compounds are bactericidal for
S. aureus
and bacteriostatic for
A. baumannii
. The probable mode of action is the disruption of the bacterial cell membrane. Furthermore, potent compounds are nontoxic to human cell lines at several fold higher concentrations than the MICs.
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