ArticleBioorganic & medicinal chemistry letters2019
Synthesis of analogs of the Gwt1 inhibitor manogepix (APX001A) and in vitro evaluation against Cryptococcus spp.
Article in Bioorganic & medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed.
- Central Nervous System Aspergillosis: Advances in Diagnosis, Therapeutics, and Multidisciplinary Management (2026 Update).Mycoses · 2026Review
- Rho2-dependent cell wall remodeling boosts the fungistatic activity of manogepix againstCell surface (Amsterdam, Netherlands) · 2026Article
- Identification of GPI-Anchored Wall Transfer Protein 1 Modulators for Fungal Infections Through Generative AI and Physics-Based Approaches.International journal of molecular sciences · 2026Article
- Novel Inositol Acyltransferase (Gwt1) Inhibitor for Fungal Keratitis Treatment: Evaluation of In Vitro and In Vivo Efficacy and Safety.Investigative ophthalmology & visual science · 2026Article
- Current and emerging therapies for fungal biofilms and systemic infections.Critical reviews in microbiology · 2026Review
- Fungal Sphingolipids: Biosynthesis Pathways, Structural Features and Biological Functions.Journal of fungi (Basel, Switzerland) · 2026Review
- Next-generation antifungal drugs: Mechanisms, efficacy, and clinical prospects.Acta pharmaceutica Sinica. B · 2025Review
- Targeting fungal lipid synthesis for antifungal drug development and potentiation of contemporary antifungals.npj antimicrobials and resistance · 2025Review
- Comparative evaluation of sensititre YeastOne and VITEK2 antifungal susceptibility tests with CLSI broth microdilution method of clinicalMicrobiology spectrum · 2025Article
- The evolution of antifungal therapy: Traditional agents, current challenges and future perspectives.Current research in microbial sciences · 2025Review
- Fungal lung disease.The European respiratory journal · 2024Review
- Review
- Advancements and challenges in antifungal therapeutic development.Clinical microbiology reviews · 2024Review
- Calcineurin Inhibitors Synergize with Manogepix to Kill Diverse Human Fungal Pathogens.Journal of fungi (Basel, Switzerland) · 2022Article
- Advances in anti-fungal therapies.Mycopathologia · 2021Review
- Antifungal Pipeline.Frontiers in cellular and infection microbiology · 2021Review
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
Fosmanogepix (APX001) is a first-in-class prodrug molecule that is currently in Phase 2 clinical trials for invasive fungal infections. The active moiety manogepix (APX001A) inhibits the novel fungal protein Gwt1. Gwt1 catalyzes an early step in the GPI anchor biosynthesis pathway. Here we describe the synthesis and evaluation of 292 new and 24 previously described analogs that were synthesized using a series of advanced intermediates to allow for rapid analoging. Several compounds demonstrated significantly (8- to 32-fold) improved antifungal activity against both Cryptococcus neoformans and C. gattii as compared to manogepix. Further in vitro characterization identified three analogs with a similar preliminary safety and in vitro profile to manogepix and superior activity against Cryptococcus spp.
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Registered trials
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