Abstract

Antibiotic resistance is a global problem, and one promising solution to overcome this issue is using metallodrugs, which are drugs containing metal ions and ligands. These complexes are superior to free ligands in various characteristics including anticancer properties and mechanism of action. The pharmacological potential of metallodrugs can be modulated by the appropriate selection of ligands and metal ions. A good example of proper coordination is the combination of sulfonamides (sulfamerazine, sulfathiazole) with a ruthenium(III) ion. This work aimed to confirm that the activity of sulfonamides antibacterial drugs is initiated and/or stimulated by their coordination to an Ru(III) ion. The study determined the structure, electrochemical profile, CT-DNA affinity, and antimicrobial as well as anticancer properties of the synthesized complexes. The results proved that Ru(III) complexes exhibited better biological properties than the free ligands.

Highlights

  • Modern antibiotic therapy has proven unsatisfactory in recent years

  • The first one corresponds to their structures as representatives of the class of sulfonamides antibacterial drugs. This finding suggests that STZ and SMZ can be simple and useful models for improving the biological and chemical changes resulting from coordination with refluxing the 1:2 (Ru)(III) and the formation of adequate, stable complexes

  • The second role corresponds to their nature as sulfonamides ligands (Figure 2A,B) having an affinity for Ru(III) ions, which may allow creating a sulfamide-ruthenium drug (Figure 2C,D) with a significantly increased therapeutical index compared to the original sulfa-ligand

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Summary

Introduction

Modern antibiotic therapy has proven unsatisfactory in recent years. Antibiotics were first used as growth promoters in farm animals in the early 20th century, which led to their introduction into the daily human diet. A serious, previously unanticipated phenomenon emerged—the development of microbial resistance to antibiotics [1]. Antibiotic resistance accounts for 2.8 million infections in the USA every year. More than 35,000 of these infections result in death [2]. Bacteria have developed resistance to a wide range of antibiotics, including sulfonamides (Figure 1A)

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