Abstract
Series of new thiazolidine-2,4-dione-based chlorophenylthiosemicarbazone hybrids (17–40) were synthesized by the reaction of condensation chlorophenylthiosemicarbazides with formylphenyl 2-(2,4-dioxothiazolidin-5-yl/ylidene)acetates. New compounds were tested on reference strains of Gram-positive and Gram-negative bacteria. The antibacterial activity of target compounds was determined by broth dilution method. Most active compounds possess minimum inhibitory concentration (MIC) = 3.91 mg/L. These compounds were non-toxic at concentrations close to their antibacterial effect. The antibacterial activity of some compounds was similar to or higher than the activity of used reference drugs such as oxacillin and cefuroxime. The structure–activity relationships (SARs) analysis collectively suggests that at least two different molecular mechanisms of their antibacterial activity should be expected.
Highlights
The appearance of drug-resistant strains of pathogenic microorganisms is a serious medical problem in worldwide
Substances with an N-N-C(=S)-N structural fragment exhibit antimicrobial activity at low non-toxic concentrations
Our research group was focused on developing new antibacterial agents composed of three-core
Summary
The appearance of drug-resistant strains of pathogenic microorganisms is a serious medical problem in worldwide. There is an urgent need to discover novel effective antimicrobial agents. Discovery of new compounds with antimicrobial activity or finding new mechanisms of action for known compounds is an important task of medicinal chemistry [1]. The 4-thiazolidinone derivatives and their narrow group—thiazolidine-2,4-diones (TZDs)—are the object of special scientific studies. This is confirmed by numerous reviews [2,3,4,5,6]. This attention is due to the wide possibilities for chemical modification of these derivatives, and to a diverse spectrum of pharmacological properties and affinity for various biological targets
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