Abstract

Aims: To explore the antifungal activity of 2,3-dimethylquinoxaline.
 Study Design: A preclinical study of a compound against 10 fungal species.
 Backgrounds: Severe fungal infections cause significant clinical problem and need more effort to search for new antifungals.
 Methodology: We evaluated the susceptibility of 2,3-dimethylquinoxaline in vitro against a wide range of pathogenic fungi, including six Candida species, two Aspergillus species, one Cryptococcus species, and one Trichophyton species. Also, we evaluated the susceptibility of 2,3-dimethylquinoxaline in vivo against oral candidiasis using a mice model.
 Results: The highest score of the minimum inhibitory concentration was 9 µg/ml against Cryptococcus neoformans. While, the lowest score was 1125 µg/ml against Candida tropicalis. The oral candidiasis in a mouse model was resolved using 2,3-dimethylquinoxaline 1% gel.
 Conclusion: The 2,3-Dimethyquinoxaline has interesting antifungal activity. Quinoxalines in general need to be further developed as a promising antifungal candidate.

Highlights

  • Fungal infections significantly affect human health, with disease severity ranging from mild unpleasant superficial infections to severe lifethreatening invasive infections [1,2]

  • We evaluated the susceptibility of 2,3-dimethylquinoxaline in vitro against a wide range of pathogenic fungi, including six Candida species, two Aspergillus species, one Cryptococcus species, and one Trichophyton species

  • It was observed that at day three post-infection, there was an apparent reduction of the infection severity in mice treated with 2,3dimethylquinoxaline 1% gel compared to the control group

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Summary

Introduction

Fungal infections significantly affect human health, with disease severity ranging from mild unpleasant superficial infections to severe lifethreatening invasive infections [1,2]. Severe infections are rising in parallel with an expanding population at high-risk, including transplantation, cancer, immunodeficiency, and critically ill patients [1]. Fungal infection includes a wide range of diseases and requires prolong treatment [2]. Aspergillus, Candida, and Cryptococcus are the most common life-threatening infection in humans [2]. Invasive aspergillosis is a progressive disease, often fatal in transplant recipients and critically ill patients [3]. Candidemia is a common bloodstream infection associated with a high mortality rate [4]. Cryptococcosis caused thousands of deaths annually among the papulation of immunocompromised [5]

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