The Synthesis of Triazolium Salts as Antifungal Agents: A Biological and In Silico Evaluation
Serghei Pogrebnoi,
Oleg Radul,
Eugenia Stingaci,
Lucian Lupascu,
Vladimir Valica,
Livia Uncu,
Anastasia Smetanscaia,
Anthi Petrou,
Ana Ćirić,
Jasmina Glamočlija,
Marina Soković,
Athina Geronikaki,
Fliur Z. Macaev
Affiliations
Serghei Pogrebnoi
Laboratory of Organic Synthesis, Institute of Chemistry, 3 Str. Academiei, MD-2028 Chisinau, Moldova
Oleg Radul
Laboratory of Organic Synthesis, Institute of Chemistry, 3 Str. Academiei, MD-2028 Chisinau, Moldova
Eugenia Stingaci
Laboratory of Organic Synthesis, Institute of Chemistry, 3 Str. Academiei, MD-2028 Chisinau, Moldova
Lucian Lupascu
Laboratory of Organic Synthesis, Institute of Chemistry, 3 Str. Academiei, MD-2028 Chisinau, Moldova
Vladimir Valica
Scientific Center for Drug Research, “Nicolae Testemitanu” State University of Medicine and Pharmacy, MD-2004 Chisinau, Moldova
Livia Uncu
Scientific Center for Drug Research, “Nicolae Testemitanu” State University of Medicine and Pharmacy, MD-2004 Chisinau, Moldova
Anastasia Smetanscaia
Scientific Center for Drug Research, “Nicolae Testemitanu” State University of Medicine and Pharmacy, MD-2004 Chisinau, Moldova
Anthi Petrou
Department of Pharmacy School of Health, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Ana Ćirić
Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research, Siniša Stanković, University of Belgrade, Bulevar Despota Stefana 142, 11000 Belgrade, Serbia
Jasmina Glamočlija
Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research, Siniša Stanković, University of Belgrade, Bulevar Despota Stefana 142, 11000 Belgrade, Serbia
Marina Soković
Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research, Siniša Stanković, University of Belgrade, Bulevar Despota Stefana 142, 11000 Belgrade, Serbia
Athina Geronikaki
Department of Pharmacy School of Health, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Fliur Z. Macaev
Laboratory of Organic Synthesis, Institute of Chemistry, 3 Str. Academiei, MD-2028 Chisinau, Moldova
The control of fungal pathogens is increasingly difficult due to the limited number of effective drugs available for antifungal therapy. In addition, both humans and fungi are eukaryotic organisms; antifungal drugs may have significant toxicity due to the inhibition of related human targets. Furthermore, another problem is increased incidents of fungal resistance to azoles, such as fluconazole, ketoconazole, voriconazole, etc. Thus, the interest in developing new azoles with an extended spectrum of activity still attracts the interest of the scientific community. Herein, we report the synthesis of a series of triazolium salts, an evaluation of their antifungal activity, and docking studies. Ketoconazole and bifonazole were used as reference drugs. All compounds showed good antifungal activity with MIC/MFC in the range of 0.0003 to 0.2/0.0006–0.4 mg/mL. Compound 19 exhibited the best activity among all tested with MIC/MFC in the range of 0.009 to 0.037 mg/mL and 0.0125–0.05 mg/mL, respectively. All compounds appeared to be more potent than both reference drugs. The docking studies are in accordance with experimental results.
