Pogrebnoi Serghei, Radul Oleg, Stingaci Eugenia, Lupascu Lucian, Valica Vladimir, Uncu Livia, Smetanscaia Anastasia, Petrou Anthi, Ćirić Ana, Glamočlija Jasmina, Soković Marina, Geronikaki Athina, Macaev Fliur Z
Laboratory of Organic Synthesis, Institute of Chemistry, 3 Str. Academiei, MD-2028 Chisinau, Moldova.
Scientific Center for Drug Research, "Nicolae Testemitanu" State University of Medicine and Pharmacy, MD-2004 Chisinau, Moldova.
Antibiotics (Basel). 2022 Apr 27;11(5):588. doi: 10.3390/antibiotics11050588.
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 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.
由于抗真菌治疗可用的有效药物数量有限,控制真菌病原体变得越来越困难。此外,人类和真菌都是真核生物;抗真菌药物可能因抑制相关人类靶点而具有显著毒性。此外,另一个问题是真菌对唑类药物(如氟康唑、酮康唑、伏立康唑等)的耐药性事件增加。因此,开发具有更广泛活性谱的新型唑类药物仍然吸引着科学界的关注。在此,我们报告了一系列三唑鎓盐的合成、它们的抗真菌活性评估以及对接研究。酮康唑和联苯苄唑用作参考药物。所有化合物均表现出良好的抗真菌活性,MIC/MFC范围为0.0003至0.2/0.0006 - 0.4 mg/mL。化合物 在所有测试化合物中表现出最佳活性,MIC/MFC分别在0.009至0.037 mg/mL和0.0125 - 0.05 mg/mL范围内。所有化合物似乎都比两种参考药物更有效。对接研究与实验结果一致。