Synthesis and in vitro antifungal evaluation of 2-(2,4-difluorophenyl)-1- [(1H-indol-3-ylmethyl)methylamino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols

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Abstract

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 381.0ng/mL) suggesting an inhibition of 14α-demethylase by sterol analysis studies, but are weaker inhibitors compared to their indol-5-ylmethylamino analogs. © 2011 Informa UK, Ltd.

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Guillon, R., Logé, C., Pagniez, F., Ferchaud-Roucher, V., Duflos, M., Picot, C., & Pape, P. L. (2011). Synthesis and in vitro antifungal evaluation of 2-(2,4-difluorophenyl)-1- [(1H-indol-3-ylmethyl)methylamino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols. Journal of Enzyme Inhibition and Medicinal Chemistry, 26(2), 261–269. https://doi.org/10.3109/14756366.2010.503607

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