In vitro antifungal activity of new series of homoallylamines and related compounds with inhibitory properties of the synthesis of fungal cell wall polymers

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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2003-04, Vol.11 (7), p.1531-1550
Main Authors: VARGAS M, Leonor Y, CASTELLI, Maria V, KOUZNETSOV, Vladimir V, URBINA G, Juan M, LOPEZ, Silvia N, SORTINO, Maximiliano, ENRIZ, Ricardo D, RIBAS, Juan C, ZACCHINO, Susana
Format: Article
Language:English
Subjects:
Allylamine - analogs & derivatives
Allylamine - chemical synthesis
Allylamine - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal agents
Antifungal Agents - chemical synthesis
Antifungal Agents - pharmacology
Arthrodermataceae - drug effects
Biological and medical sciences
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
Medical sciences
Microbial Sensitivity Tests
Pharmacology. Drug treatments
Saccharomyces cerevisiae - drug effects
Saccharomyces cerevisiae - enzymology
Structure-Activity Relationship
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Summary: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.
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(02)00605-3