Abstract
The synthesis, in vitro antifungal evaluation and SAR studies of 101 compounds of the 4-aryl-, 4-alkyl-, 4-pyridyl or -quinolinyl-4-N-arylamino-1-butenes series and related compounds, are reported here. Active structures showed to inhibit (1,3)-beta-D-glucan and mainly chitin synthases, enzymes that catalyze the synthesis of the major fungal cell wall polymers.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Allylamine / analogs & derivatives*
-
Allylamine / chemical synthesis*
-
Allylamine / pharmacology*
-
Antifungal Agents / chemical synthesis*
-
Antifungal Agents / pharmacology*
-
Arthrodermataceae / drug effects
-
Cell Wall / drug effects*
-
Chitin Synthase / antagonists & inhibitors
-
Computational Biology
-
Enzyme Inhibitors / chemical synthesis
-
Enzyme Inhibitors / pharmacology
-
Fungi / cytology
-
Fungi / drug effects*
-
Glucosyltransferases / antagonists & inhibitors
-
Indicators and Reagents
-
Microbial Sensitivity Tests
-
Saccharomyces cerevisiae / drug effects
-
Saccharomyces cerevisiae / enzymology
-
Structure-Activity Relationship
Substances
-
Antifungal Agents
-
Enzyme Inhibitors
-
Indicators and Reagents
-
Allylamine
-
Glucosyltransferases
-
glucan synthase
-
Chitin Synthase