4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 2, Pages 301-304

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.11.101

Keywords

Homology model; Docking; H-bond acceptor; Triazole; Candida albicans; CYP51 inhibitors; Antifungal agents

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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 Candida albicans. These results confirmed both the importance of pi-pi stacking and hydrogen bonding interactions in the active site of CYP51-C. albicans. (C) 2008 Elsevier Ltd. All rights reserved.

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