Antimicrobial activity evaluation of N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives

Antibiotic resistance is currently a global problem for modern civilization. Microorganisms become resistant to drugs through acquired mechanisms. Six pathogens are responsible for the majority of deaths: Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae, Streptococcus pneumoniae, Acinetobacter baumannii and Pseudomonas aeruginosa. Growing drug resistance makes basic antibiotic therapy ineffective and increases the costs of polytherapy [1]. In recent years, there has been increasing interest in organic compounds that contain an aryl or a heteroarylsulfonamide group in their structure, which are characterized not only by anticancer activity but also by antimicrobial activity [2]. The presented studies follow the trend of searching for new hybrid molecules resulting from the combination of different pharmacophores with interesting biological profiles.

The antibacterial activity of compounds that had previously shown interesting anticancer activity was assessed [3]. The compounds were subjected to an assessment of their antibacterial activity in in vitro tests against the Gram-positive bacterium Staphylococcus aureus (MIC = 8 µg/mL) and the Gram-negative Escherichia coli (MIC > 125 µg/mL). The most active derivative (16) was tested against the Gram-positive bacteria S. epimermidis, E. faecalis, and B. subtilis (MICs in a range from 2 to 125 µg/mL) and clinical strains of MRSA (MICs between 0.5 and 1 µg/mL). Ampicillin was used as the standard. The activity of the tested compound against a bacterial biofilm was also tested, and its hemolytic activity was assessed in the peripheral blood of domestic sheep.

References:

[1] Uddin T. M., Chakraborty A. J., Khusro A., Zidan R. M., Mitra S., Emran T. B., Dhama K., Ripon K. H., Gajdács M., Sahibzada M. U. K., Hossain J.; J. Infect. Public Health (2021), 14 (12), 1750.

[2] Verma S. K., Verma R., Xue F., Thakur P. K., Girish Y. R., Rakesh K. P.; Bioorg. Chem. (2020), 105, 104400.

[3] Bułakowska A., Sławiński J., Siedlecka-Kroplewska K., Stasiłojć G., Serocki M., Heldt M., Bioorg. Chem. (2020), 104, 10430.