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Antimicrobial Synergy Testing by the Inkjet Printer-assisted Automated Checkerboard Array and the Manual Time-kill Method
Published on: April 18, 2019
New systematically active antimycotics from the beta-blocker category
H Hänel1, R Kirsch, H L Schmidts
1Hoechst AG, Frankfurt/Main, Germany.
Mycoses
|July 1, 1995
Summary
New beta-blocker-like compounds show significant antifungal activity against Candida albicans. These novel antimycotics effectively inhibit fungal cell penetration and protect mice in vivo.
Area of Science:
- Mycology
- Pharmacology
- Medicinal Chemistry
Background:
- Candida albicans secretes phospholipases, crucial for fungal cell penetration.
- Lipophilic beta-blocking structures are known inhibitors of mammalian phospholipases.
Purpose of the Study:
- To synthesize and evaluate novel beta-hydroxyethylamine derivatives as potential antimycotics.
- To assess the in vitro and in vivo efficacy of these compounds against Candida albicans.
Main Methods:
- Synthesis of beta-hydroxyethylamine derivatives.
- In vitro antifungal assays against Candida albicans.
- In vivo studies using a murine model of invasive candidiasis.
- Histological examination of tissue penetration.
Main Results:
- Several synthesized compounds demonstrated broad in vitro antifungal activity.
- In combination with fluconazole, these compounds significantly reduced mortality in infected mice.
- Histological analysis confirmed inhibition of fungal tissue penetration by the novel compounds.
Conclusions:
- Beta-blocker-like structures derived from beta-hydroxyethylamines represent a new class of antimycotics.
- These compounds exhibit potent in vitro and in vivo efficacy against Candida albicans.
- They effectively inhibit fungal cell penetration, offering a promising therapeutic strategy.
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