Abstract
A new complex of Bi(III) and sulfapyridine was synthesized and characterized by elemental analysis, atomic absorption spectrometry, conductivity analysis, electrospray ionization mass spectrometry (ESI-MS), infrared spectroscopy, and single crystal X-ray diffraction methods. The antimicrobial and the cytotoxic activities of the compound were investigated. Elemental and conductivity analyses are in accordance to the formulation [BiCl3(C11H11N3O2S)3]. The structure of the complex reveals a distorted octahedral geometry around the bismuth atom, which is bound to three sulfonamidic nitrogens from sulfapyridine, acting as a monodentate ligand, and to three chloride ions. The presence of the compound in solution was confirmed by ESI-MS studies. The complex is 3 times more potent than the ligand against Salmonella typhimurium, 4 times against Staphylococcus aureus, Shigella dysenteriae, and Shigella sonnei and 8 times more potent against Pseudomonas aeruginosa and Escherichia coli. The compound inhibits the growth of chronic myelogenous leukemia cells with an IC50 value of 44 μM whereas the free ligand has no effect up to 100 μM.
Highlights
The excessive use of antibiotics caused the emergence of drug-resistant bacterial strains through a variety of mechanisms
The mode of action of sulfonamides involves the disruption of bacterial folic acid synthesis, which is essential for the biosynthesis of
Sulfapyridine mimics the paraaminobenzoic acid (PABA), which is a natural substrate required for the biosynthesis of folic acid
Summary
The excessive use of antibiotics caused the emergence of drug-resistant bacterial strains through a variety of mechanisms. This problem has become quite alarming because almost all pathogenic bacteria have acquired resistance against the presently known and widely used antibiotics [1,2,3]. Sulfonamides were the first synthetic antibiotics to be used in clinic and they exhibit interesting pharmacological properties, such as selectivity to bacterial cells and low toxicity. The competition between sulfapyridine and PABA for the enzyme results in sulfapyridine binding, because it possesses a greater affinity for the enzyme This inhibits the enzyme activity and the biosynthesis of folic acid [4]. Bismuth compounds have been used for centuries in the treatment of a variety of microbial infections due to their high efficacy and low toxicity. We have synthesized, characterized and studied the antimicrobial and cytotoxic activities of a new compound of bismuth(III) and sulfapyridine
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