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Arzneimittelforschung ; 53(10): 738-43, 2003.
Article in English | MEDLINE | ID: mdl-14650367

ABSTRACT

The synthesis, in vitro/in vivo antifungal evaluation and a structure-activity relationship (SAR) study of 3(2H)-pyridazinones was carried out. The results reported here may be helpful in the structural identification and understanding of the minimum structural requirements for these molecules acting as antifungal agents. In addition, the most active structure in this series was tested for its capacity of inhibiting Saccharomyces cerevisiae beta 1,3-glucan synthase and chitin synthase, enzymes that catalyze the synthesis of the major polymers of the fungal cell wall.


Subject(s)
Antifungal Agents/chemical synthesis , Antifungal Agents/pharmacology , Fungi/drug effects , Pyridazines/chemical synthesis , Pyridazines/pharmacology , Administration, Topical , Animals , Arthrodermataceae/drug effects , Chitin Synthase/antagonists & inhibitors , Dermatomycoses/drug therapy , Dermatomycoses/microbiology , Guinea Pigs , Indicators and Reagents , Ketoconazole/pharmacology , Male , Microbial Sensitivity Tests , Saccharomyces cerevisiae/drug effects , Saccharomyces cerevisiae/enzymology , Structure-Activity Relationship
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