Abstract
A series of novel pyrazino[2,1-a]isoquinolin compounds were designed, synthesized, and their antifungal activities in vitro were evaluated. The results showed that all of the title compounds exhibited antifungal activities. Most of them exhibited stronger antifungal activities than the lead compounds; compound 7c is more potent than fluconazole against two of the three tested fungal strains. The studies presented here provide a new structural type for the development of novel antifungal agents.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antifungal Agents / chemical synthesis*
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacology
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Candida / drug effects
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Candida / enzymology
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Cryptococcus neoformans / drug effects
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Cryptococcus neoformans / enzymology
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Cytochrome P-450 Enzyme Inhibitors
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Drug Design*
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Fungi / drug effects
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Fungi / enzymology
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Isoquinolines / chemical synthesis*
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Isoquinolines / chemistry
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Isoquinolines / pharmacology
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Microbial Sensitivity Tests
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Models, Molecular
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Molecular Structure
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Pyrazines / chemical synthesis*
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Pyrazines / chemistry
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Pyrazines / pharmacology
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Sterol 14-Demethylase
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Trichophyton / drug effects
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Trichophyton / enzymology
Substances
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Antifungal Agents
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Cytochrome P-450 Enzyme Inhibitors
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Isoquinolines
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Pyrazines
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Sterol 14-Demethylase