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

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 Candi...

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Veröffentlicht in:Journal of enzyme inhibition and medicinal chemistry 2011-04, Vol.26 (2), p.261-269
Hauptverfasser: Guillon, Rémi, Logé, Cédric, Pagniez, Fabrice, Ferchaud-Roucher, Véronique, Duflos, Muriel, Picot, Carine, Pape, Patrice Le
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Sprache:eng
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Zusammenfassung: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.
ISSN:1475-6366
1475-6374
DOI:10.3109/14756366.2010.503607