Abstract
Rising resistance of pathogenic bacteria reduces the options of treating hospital and non-hospital bacterial infections. There is a need to search for newer chemotherapies that will show antimicrobial ability against planktonic cells as well as bacterial biofilms. We have synthesized a series of N-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)amides, namely, molecular hybrids, which include a 2-mercaptobenzenosulfonamide fragment and either cinnamic or cyclohexylpropionic acid residues. The antimicrobial activity of compounds 8–17 was evaluated on Gram-positive, Gram-negative bacteria and fungal species. Experiments took into account investigation of antibacterial activity against planktonic cells as well as biofilms. Compounds 8–17 showed high bacteriostatic activity against staphylococci, with the most active molecules 10 and 16 presenting low MIC values of 4–8 μg/mL against reference methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive S. aureus (MSSA) strains as well as clinical isolates. Compounds 10 and 16 also showed an ability to inhibit biofilms formed by MRSA and MSSA. The potential of 10 and 16 as antibiofilm agents was supported by cytotoxicity assays that indicated no cytotoxic effect either on normal cells of human keratinocytes or on human cancer cells, including cervical, colon, and breast cancer lines.
Highlights
An increasing resistance of pathogenic bacteria towards existing antibiotics is a global therapeutic problem, affecting both hospital and non-hospital infections
We proved that 4-chloro-2-mercapto-5-methylbenzenesulfonamides show a wide range of antibacterial activity against numerous bacterial strains obtained from patients with infections of the oral cavity: gingivitis, periodontal diseases, corrosive ulcers, stomatitis, respiratory tract, or intestinal tract [10,11]
The aim of the present study was to evaluate a group of N-(2-arylmethylthio-4-chloro-5methylbenzenesulfonyl)amides as potential antimicrobial agents exhibiting bacteriostatic/bactericidal activity against planktonic bacterial cells as well as antibiofilm activity against structures formed by some strains associated with biofilm-related diseases
Summary
An increasing resistance of pathogenic bacteria towards existing antibiotics is a global therapeutic problem, affecting both hospital and non-hospital infections. In 2018, the rise of resistant strains was considered by the World Health Organization (WHO) to be a global concern [1]. One of the main causes of antibiotic resistance is abuse and misuse of drugs by patients. Use of huge amounts of antibiotics over the past 75 years has made almost all pathogenic bacteria resistant to common antibiotics [2]. As a result of this process, the number of multidrug resistant strains, insensitive to commercial treatments, is still growing [3]. Rising resistance reduces the options of treating bacterial infections in hospital interventions, including surgery, transplantation, and chemotherapy. The resistance mentioned above is not completely explicated by the rise of resistant strains and by the formation of biofilms by bacteria
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