title: 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.
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 381.0 ng/mL) suggesting an inhibition of 14α-demethylase by sterol analysis studies, but are weaker inhibitors compared to their indol-5-ylmethylamino analogs.
authors.affiliation: 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.
authors.forename: Rémi
authors.initials: R
authors.lastname: Guillon
authors.forename: Cédric
authors.initials: C
authors.lastname: Logé
authors.forename: Fabrice
authors.initials: F
authors.lastname: Pagniez
authors.forename: Véronique
authors.initials: V
authors.lastname: Ferchaud-Roucher
authors.forename: Muriel
authors.initials: M
authors.lastname: Duflos
authors.forename: Carine
authors.initials: C
authors.lastname: Picot
authors.forename: Patrice
authors.initials: P
authors.lastname: Le Pape
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects*; D020134:Catalytic Domain; D015195:Drug Design; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D020005:Propanols / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D020005:Propanols; D014230:Triazoles