Université de Nantes, Nantes Atlantique Universités, Département de Pharmacochimie, Cibles et Médicaments des Infections, de l'Immunité et du Cancer, IICIMED-EA 1155, UFR Sciences Pharmaceutiques, Nantes, France.
J Enzyme Inhib Med Chem. 2011 Apr;26(2):261-9. doi: 10.3109/14756366.2010.503607. Epub 2010 Aug 9.
We extended our previous studies based on the design of 1-[(1H-indol-5-ylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents toward the identification of new indol-3-ylmethylamino derivatives. The majority of these compounds exhibited antifungal activity against a Candida albicans strain (minimum inhibitory concentrations ranging from 199.0 to 381.0 ng/mL) suggesting an inhibition of 14α-demethylase by sterol analysis studies, but are weaker inhibitors compared to their indol-5-ylmethylamino analogs.
我们基于 1-[(1H-吲哚-5-基甲基)氨基]-2-苯基-3-(1H-1,2,4-三唑-1-基)丙-2-醇类抗真菌药物的设计，进行了进一步的研究，以鉴定新的吲哚-3-基甲基氨基衍生物。这些化合物中的大多数对白色念珠菌菌株表现出抗真菌活性（最低抑制浓度范围为 199.0 至 381.0ng/mL），这表明甾醇分析研究中 14α-脱甲基酶受到抑制，但与它们的吲哚-5-基甲基氨基类似物相比，它们的抑制作用较弱。
