Department of Biomedical and Biotechnological Sciences, Microbiology Section, University of Catania, Catania, Italy.
Department of Chemical Sciences, University of Catania, Catania, Italy.
Nat Prod Res. 2020 Jun;34(12):1653-1662. doi: 10.1080/14786419.2018.1525375. Epub 2018 Nov 13.
In this work we synthetized the bioinspired benzoxanthene lignans (BXLs) , , and the phenazine derivative as potential antimycotic agents. MICs and MFCs against strains were determined. In a preliminary screening, compounds , , , , were substantially inactive. Compounds and showed antifungal activity, being able to inhibit the growth of the majority of strains with MIC values in the range 4.6-19.2 µM () and 26.0-104.3 µM (); for three strains, the MICs were lower than those obtained using the antimycotic drug fluconazole. The three BXLs , and showed some MIC values lower than that of fluconazole; was also active against two non strains resistant to fluconazole. Phenazine , although active only against one strain (MIC = 1.3 µM), was one order of magnitude more potent than fluconazole. All the BXLs were fungicidal.
在这项工作中，我们合成了受生物启发的苯并氧杂蒽木脂素（BXLs）[1-3]和吩嗪衍生物[4]，作为潜在的抗真菌剂。测定了它们对[5]株的最小抑菌浓度（MIC）和最小杀菌浓度（MBC）。在初步筛选中，化合物[1-3]、[4]、[5]、[6]、[7]基本没有活性。化合物[8]和[9]表现出抗真菌活性，能够抑制大多数[5]株的生长，MIC 值在 4.6-19.2 μM（[8]）和 26.0-104.3 μM（[9]）范围内；对三种菌株，MIC 值低于抗真菌药物氟康唑的 MIC 值。三种 BXLs[8]、[9]和[10]的一些 MIC 值低于氟康唑；[10]对两种耐氟康唑的非[5]株也有活性。吩嗪[4]虽然仅对一株菌（MIC=1.3 μM）有效，但比氟康唑的活性高一个数量级。所有 BXLs 均具有杀菌作用。
