Session: Heterocycles & Aromatics:

The development of a cancer therapeutic that not only possesses antiproliferative abilities but also exhibits effective antimicrobial activity has increased in importance due to patients' compromised immune systems. N,N’-bis-substituted triazolium salts have begun to demonstrate their biological activity. Literature has shown the anti-proliferative ability of N,N’-bis-substituted-1,2,4 triazolium salts against prostate (PC-3) and breast cancer (MDA-MB-468) cell lines.2 Similar in structure, 1,2,3 triazolium salts have shown promising bactericidal effects and were more effective in comparison to the 1,2,4-triazolium parent.3 An investigation into the structure activity relationship (SAR) between substituents and antimicrobial ability has noted the naphthylmethyl substituent most successful when produced in a symmetric form. This has encouraged an investigation into the development and testing of asymmetric N,N’-bis-substituted-1,2,3 triazolium salts for effective antimicrobial activity. Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species (ESKAPE) are the most common pathogens contributing to infections in the clinical setting. In order to fully understand the utility of the triazole ring as an antimicrobial agent, we present a structure activity relationship of N,N’-bis-substituted 1,2,3-triazolium salts synthesized with varying asymmetric substituents. These novel N,N’-bis-substituted 1,2,3-triazolium salts will be synthesized, characterized, and tested for their biological activities when used as antimicrobial agents.

Lauren King

Appearances