SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium.
Bioorg Med Chem Lett. 2013 Aug 15;23(16):4641-3. doi: 10.1016/j.bmcl.2013.06.014. Epub 2013 Jun 13.
Antifungal assessment of eighteen 5-, 6- and 8-(4-aminobutyloxy)quinolines revealed a significant susceptibility of the tested fungi and yeast strains (Candida albicans, Rhodotorula bogoriensis, Aspergillus flavus and Fusarium solani) toward different halo-substituted 8-(4-aminobutyloxy)quinolines. The six most potent compounds displayed antifungal activities similar to those of established antifungal agents such as Amphotericin B, Fluconazole and Itraconazole, and one representative also showed a promising broad-spectrum antifungal profile. The introduction of an aminoalkoxy side chain at the 8-position of a halo-substituted quinoline core might thus provide a new class of lead structures in the search for novel antifungal agents.
对十八种 5-、6-和 8-（4-氨基丁氧基）喹啉进行抗真菌评估，发现测试的真菌和酵母菌株（白色念珠菌、博氏红酵母、黄曲霉和茄病镰刀菌）对不同卤代 8-（4-氨基丁氧基）喹啉具有显著的敏感性。六种最有效的化合物显示出与现有抗真菌药物（如两性霉素 B、氟康唑和伊曲康唑）相似的抗真菌活性，其中一种代表性化合物还表现出有希望的广谱抗真菌特性。因此，在寻找新型抗真菌药物时，在卤代喹啉核的 8 位引入氨基烷氧基侧链可能提供一类新的先导结构。
