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

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 MIC80 values ranging from 1410.0 to 23.0 ng mL−1 on Candidaalbicans. These results confirmed both the importance of π–π stacking and hydrogen bonding interactions in the active site of CYP51-C. albicans.

Graphical abstractSynthesis and SAR studies of modified 1-benzylamino-2-phenyl-3-(1H-1,2,4-triazol-1yl)propan-2-ols as antifungal agents, allowed identification of new derivatives with MIC80 values ranging from 1410.0 to 23.0 ng mL−1 on the Candidaalbicans strain.Figure optionsDownload full-size imageDownload as PowerPoint slide