Human fungal infections may fail to respond to contemporary antifungal therapies in vivo despite in vitro fungal isolate drug susceptibility. Such a discrepancy between in vitro antimicrobial susceptibility and in vivo treatment outcomes is partially explained by microbes adopting a drug-resistant biofilm mode of growth during infection. The filamentous fungal pathogen
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Invasive fungal infections are increasing worldwide due to an expanding number of immunocompromised patients as well as an increase in drug-resistant fungi. While fungal resistance has increased, this resistance has not been accompanied by the development of new antifungals. A common class of antifungal agents that are prescribed are the azoles, which contain either a triazole or an imidazole group. Unfortunately, current azoles, like fluconazole, have been shown to be less effective with the increase in resistant fungal pathogens. Therefore, the development of novel azole antifungal compounds is of urgent need. The objective of this research was to synthesize triazole-containing small molecules with potent antifungal activity. The scaffold of the synthesized compounds contains a triazole moiety and was synthesized via a copper-catalyzed azide-alkyne click reaction (CuAAC) between the appropriate alkyne and azide intermediates. The minimum inhibitory concentrations of these compounds were determined using standard broth microdilution assays against opportunistic bacteria and fungi associated with life-threatening invasive fungal infections. Although the synthesized compounds possessed no antimicrobial activity, these results can be used to further the long-term goal of developing and optimizing lead compounds with potent
- Award ID(s):
- 2116635
- PAR ID:
- 10549913
- Publisher / Repository:
- PeerJ
- Date Published:
- Journal Name:
- PeerJ Organic Chemistry
- Volume:
- 6
- ISSN:
- 2831-6223
- Page Range / eLocation ID:
- e10
- Format(s):
- Medium: X
- Sponsoring Org:
- National Science Foundation
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