Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Molecules. 2017 Nov 3;22(11):1895. doi: 10.3390/molecules22111895.
Fungal infections threaten human health, particularly in immune-compromised patients worldwide. Although there are a large number of antifungal agents available, the desired clinical attributes for the treatment of fungal infections have not yet been achieved. Azoles are the mainstay class of the clinically used antifungal agents. In the current study, the synthesis, spectroscopic characterization, and antifungal activity of certain new oximino ethers - bearing imidazole nuclei are reported. The ()-configuration of the imine double bond of the synthesized compounds - has been confirmed via single crystal X-ray analysis of compound as a representative example of this class of compounds. The molecular structure of compound was crystallized in the monoclinic, 2₁/, = 18.7879(14) Å, 5.8944(4) Å, = 16.7621(12) Å, = 93.063(3)°, = 1855.5(2) ų, = 4. The in vitro antifungal activity of the synthesized compounds - were evaluated using diameter of the inhibition zone (DIZ) and minimum inhibitory concentration (MIC) assays against different fungal strains. Compound manifested anti- activity with an MIC value of 0.050 µmol/mL, being almost equipotent with the reference antifungal drug fluconazole (FLC),while compounds and are the most active congeners against , being equipotent and about twenty-three times more potent than FLC with an MIC value of 0.002 µmol/mL. The results of the current report might support the development of new potent and safer antifungal azoles.
真菌感染威胁着人类健康，尤其在全球免疫功能低下的患者中更为严重。尽管有大量抗真菌药物可供使用，但尚未达到治疗真菌感染所需的理想临床特性。唑类药物是临床应用的抗真菌药物的主要类别。在目前的研究中，报告了某些新型肟醚 - 含有咪唑核的合成、光谱特征和抗真菌活性。通过代表该类化合物的化合物 的单晶 X 射线分析，证实了合成化合物中 - 亚胺双键的（）构型。化合物 的分子结构在单斜晶系中结晶， = 18.7879(14) Å, 5.8944(4) Å, = 16.7621(12) Å, = 93.063(3)°, = 1855.5(2) ų, = 4. 采用抑菌圈直径（DIZ）和最低抑菌浓度（MIC）测定法，评估了合成化合物 - 对不同真菌菌株的体外抗真菌活性。化合物 表现出抗 活性，MIC 值为 0.050 µmol/mL，与参考抗真菌药物氟康唑（FLC）几乎相当，而化合物 和 对 最为有效，MIC 值为 0.002 µmol/mL，与 FLC 相当，约为其 23 倍。本报告的结果可能支持开发新的有效和更安全的抗真菌唑类药物。
