151. Pronounced activity of aromatic selenocyanates against multidrug resistant ESKAPE bacteria
- Author
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Gniewomir Latacz, Katarzyna Kieć-Kononowicz, Małgorzata Anna Marć, Wojciech Nitek, Gabriella Spengler, Jadwiga Handzlik, Karolina Witek, Annamária Kincses, Márió Gajdács, Claus Jacob, Elżbieta Karczewska, Ahmad Yaman Abdin, Muhammad Jawad Nasim, and Ewa Żesławska
- Subjects
biology ,chemistry.chemical_element ,Context (language use) ,Biological activity ,02 engineering and technology ,General Chemistry ,Drug resistance ,010402 general chemistry ,021001 nanoscience & nanotechnology ,Antimicrobial ,biology.organism_classification ,01 natural sciences ,Catalysis ,0104 chemical sciences ,Multiple drug resistance ,chemistry ,Biochemistry ,Materials Chemistry ,0210 nano-technology ,Cytotoxicity ,Selenium ,Bacteria - Abstract
Selenocyanates represent an interesting class of organic selenium compounds. Due to their similarity with better known natural (iso-)thiocyanates, they promise high biological activity and may also be metabolized to other Reactive Selenium Species (RSeS), such as selenols, diselenides and seleninic acids. Thirteen arylmethyl selenocyanates (1–13) have been synthesized and evaluated for potential antimicrobial, nematicidal and cytotoxic activity. The compounds exhibit pronounced antimicrobial activity against various strains of Gram-positive and Gram-negative bacteria and yeasts, including multidrug resistant strains. The results obtained so far demonstrate that these arylmethyl selenocyanates are also non-mutagenic and have limited cytotoxicity against human cells. Here, benzyl selenocyanate (1) represents the most active anti-ESKAPE agent, with potent activity against multidrug resistant MRSA strains (HEMSA 5) – with a competitive MIC value of just 0.76 μg mL−1 (3.88 μM), whereas it exhibits low(er) cytotoxicity (IC50 = 31 μM) and no mutagenicity against mammalian cells. Due to this selective antimicrobial activity, aromatic selenocyanates may provide an interesting lead in the development of antimicrobial agents, particularly in the context of drug resistance.
- Published
- 2019