Abstract
We previously reported on the design and synthesis of 1-[((hetero)aryl- or piperidinylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols showing various degrees of antifungal activity against Candida albicans and Aspergillus fumigatus strains. Now we have identified a series of 1-[(1H-indol-5-ylmethyl)amino] derivatives which exhibited potent MICs (<65 ng mL(-1)) against C. albicans strain. The synthesis and SAR behind the indole scaffold will be discussed.
MeSH terms
-
Antifungal Agents / chemical synthesis*
-
Antifungal Agents / chemistry
-
Antifungal Agents / pharmacology
-
Binding Sites
-
Candida albicans / drug effects
-
Computer Simulation
-
Cytochrome P-450 Enzyme Inhibitors
-
Cytochrome P-450 Enzyme System / metabolism
-
Drug Design
-
Fungal Proteins / antagonists & inhibitors
-
Fungal Proteins / metabolism
-
Propanols / chemical synthesis*
-
Propanols / chemistry
-
Propanols / pharmacology
-
Structure-Activity Relationship
-
Triazoles / chemical synthesis*
-
Triazoles / chemistry
-
Triazoles / pharmacology
Substances
-
Antifungal Agents
-
Cytochrome P-450 Enzyme Inhibitors
-
Fungal Proteins
-
Propanols
-
Triazoles
-
cytochrome P-450 CYP51, Candida albicans
-
Cytochrome P-450 Enzyme System