College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, Nanjing 210009, China.
Bioorg Med Chem Lett. 2012 Jul 15;22(14):4887-90. doi: 10.1016/j.bmcl.2012.05.070. Epub 2012 May 24.
In an attempt to search for many target compounds with excellent activities, a series of vinyl ether-containing azole derivatives were designed, synthesized, and evaluated as antifungal agents. Results of preliminary antifungal tests against Trichophyton rubrum in vitro indicated that most of the synthesized compounds showed excellent activities. In comparison with fluconazole, itraconazole, voriconazole, omoconazole and amphotericin B, several compounds (such as 7d, 7g and 7h) exhibited more potent inhibitory activities, suggesting that they were promising leads for the development of novel antifungal agents.
为了寻找具有优异活性的多种目标化合物，设计、合成并评价了一系列含乙烯基醚的唑类衍生物作为抗真菌剂。初步的体外抗红色毛癣菌试验结果表明，大多数合成化合物表现出优异的活性。与氟康唑、伊曲康唑、伏立康唑、奥莫康唑和两性霉素 B 相比，几种化合物（如 7d、7g 和 7h）表现出更强的抑制活性，这表明它们是开发新型抗真菌剂的有希望的先导化合物。
