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Updated: Jul 29, 2025

Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds
Published on: February 14, 2018
Antifungal properties of (2S, 4R)-Ketoconazole sulfonamide analogs
Benjamin E Blass1, Sumant Puri2, Rishabh Sharma2
1Department of Pharmaceutical Sciences, Temple University School of Pharmacy, Philadelphia, PA, United States.
Abstract:
Invasive candidiasis remains a significant health concern, as it is associated with a high mortality risk. In addition, the risk of infection is significantly elevated in immunocompromised patients such as those with HIV, cancer, or those taking imcmunosuppressive drugs as a result of organ transplantation. The majority of these cases are caused by C. albicans, and C. glabrata is the second most common cause. These infections are typically treated using approved antifungal agents, but the rise of drug-resistant fungi is a serious concern. As part of our on-going effort to identify novel antifungal agents, we have studied the in vitro antifungal properties of a series of sulfonamide analogs of (2S, 4R)-Ketoconazole. Herein we report on the in vitro activity against the key fungal pathogens C. albicans, and C. glabrata.
Insights
Researchers investigated novel sulfonamide analogs of ketoconazole for antifungal properties. These compounds show potential for treating invasive candidiasis caused by drug-resistant Candida species.
Area of Science:
- Medical Mycology
- Medicinal Chemistry
Background:
- Invasive candidiasis presents a high mortality risk, particularly in immunocompromised individuals.
- Candida albicans and Candida glabrata are leading causes of invasive candidiasis.
- Increasing antifungal drug resistance necessitates the development of novel therapeutic agents.
Purpose of the Study:
- To evaluate the in vitro antifungal activity of novel sulfonamide analogs of (2S, 4R)-Ketoconazole.
- To identify potential new treatments against key Candida pathogens.
Main Methods:
- Synthesis and in vitro testing of a series of sulfonamide analogs.
- Antifungal susceptibility testing against Candida albicans and Candida glabrata.
Main Results:
- The study reports on the in vitro antifungal activity of the synthesized compounds.
- Specific activity data against C. albicans and C. glabrata are presented.
Conclusions:
- The novel sulfonamide analogs demonstrate in vitro antifungal potential.
- These compounds represent a promising starting point for developing new agents against invasive candidiasis.
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