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Updated: Oct 25, 2026

Preparation of N-(2-alkoxyvinyl)sulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
Structure-Activity Relationship Profiling of Substituted N-Phthalimidopiperidine Analogs as Broad-Spectrum Antifungal
Matthew P Dupuis1, Nour M Alkashef2, Roman A Matamoros1
1Department of Chemistry and VT Center for Drug Discovery, Virginia Tech, Blacksburg, Virginia24061, United States.
Abstract:
Invasive fungal infections are a major and escalating global health concern, frequently resulting in life-threatening systemic infection. The combination of limited therapeutic options, increasing mortality, and the rapid emergence of multidrug-resistant fungal pathogens highlights the critical need for novel antifungal agents. With this goal in mind, a high-throughput screening assay identified SLB1122168, and a subsequent structure-activity relationship study led to more potent analogs, including SSD2032594, which demonstrated fungicidal activity with a minimum inhibitory concentration of 1-4 μg/mL against Candida auris, Cryptococcus neoformans, Aspergillus fumigatus, and Mucormycosis-causing species. Additionally, SSD2032594 showed potent activity against mature biofilms of C. auris and exhibited a negligible resistance tendency in vitro. Furthermore, SSD2032594 showed a survival benefit in the Caenorhabditis elegans nematode model of C. auris infection, resulting in a ∼30% higher survival rate. Taken together, these results highlight SSD2032594 as a candidate for antifungal drug development, targeting infections caused by different fungal pathogens.
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