ArticleAntimicrobial agents and chemotherapy2013
Identification of an aminothiazole with antifungal activity against intracellular Histoplasma capsulatum.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 29 citations in OpenAlex.
- Antifungal Susceptibility Testing and Drug Discovery in the Dimorphic Fungus Histoplasma Capsulatum.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Antifungal Encapsulated into Ligand-Functionalized Nanoparticles with High Specificity for Macrophages.Pharmaceutics · 2022Article
- Evaluation of the Anti-Pharmaceutics · 2022Article
- Kinase Inhibitor Library Screening Identifies the Cancer Therapeutic Sorafenib and Structurally Similar Compounds as Strong Inhibitors of the Fungal PathogenAntibiotics (Basel, Switzerland) · 2021Article
- Peptidogalactomannan from Histoplasma capsulatum yeast cell wall: role of the chemical structure in recognition and activation by peritoneal macrophages.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2021Article
- Article
- Therapies and Vaccines Based on Nanoparticles for the Treatment of Systemic Fungal Infections.Frontiers in cellular and infection microbiology · 2020Review
- Macrophage activation by IFN-γ triggers restriction of phagosomal copper from intracellular pathogens.PLoS pathogens · 2018Article
- Synthesis and biological evaluation of aminothiazoles against Histoplasma capsulatum and Cryptococcus neoformans.Bioorganic & medicinal chemistry · 2018Article
- O-Mannosylation of Proteins EnablesmBio · 2018Article
- Eng1 and Exg8 Are the Major β-Glucanases Secreted by the Fungal PathogenThe Journal of biological chemistry · 2017Article
- Antifungal therapeutics for dimorphic fungal pathogens.Virulence · 2017Article
- Quantitative Microplate-Based Growth Assay for Determination of Antifungal Susceptibility of Histoplasma capsulatum Yeasts.Journal of clinical microbiology · 2015Article
- Design, synthesis, and biological evaluation of aminothiazole derivatives against the fungal pathogens Histoplasma capsulatum and Cryptococcus neoformans.Bioorganic & medicinal chemistry · 2015Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
As eukaryotes, fungi possess relatively few molecules sufficiently unique from mammalian cell components to be used as drug targets. Consequently, most current antifungals have significant host cell toxicity. Primary fungal pathogens (e.g., Histoplasma) are of particular concern, as few antifungals are effective in treating them. To identify additional antifungal candidates for the treatment of histoplasmosis, we developed a high-throughput platform for monitoring Histoplasma growth and employed it in a phenotypic screen of 3,600 commercially available compounds. Seven hit compounds that inhibited Histoplasma yeast growth were identified. Compound 41F5 has fungistatic activity against Histoplasma yeast at micromolar concentrations, with a 50% inhibitory concentration (IC50) of 0.87 μM, and has the greatest selectivity for yeast (at least 62-fold) relative to host cells. Structurally, 41F5 consists of an aminothiazole core with an alicyclic substituent at the 2-position and an aromatic substituent at the 5-position. 41F5 inhibits Histoplasma growth in liquid culture and similarly inhibits yeast cells within macrophages, the actual host environment of this fungal pathogen during infection. Importantly, 41F5 protects infected host cells from Histoplasma-induced macrophage death, making this aminothiazole hit compound an excellent candidate for development as an antifungal for Histoplasma infections.
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