Bioorganic & Medicinal Chemistry Letters 2009-01-15

Synthesis and structure-activity relationships of 2-phenyl-1-[(pyridinyl- and piperidinylmethyl)amino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents.

Francis Giraud, Rémi Guillon, Cédric Logé, Fabrice Pagniez, Carine Picot, Marc Le Borgne, Patrice Le Pape

Index: Bioorg. Med. Chem. Lett. 19(2) , 301-4, (2009)

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Abstract

Continuous efforts on the synthesis and structure-activity relationships (SARs) studies of modified 1-benzylamino-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents, allowed identification of new 1-[(pyridinyl- and piperidinylmethyl)amino] derivatives with MIC(80) values ranging from 1410.0 to 23.0ngmL(-1) on Candidaalbicans. These results confirmed both the importance of pi-pi stacking and hydrogen bonding interactions in the active site of CYP51-C. albicans.