ArticleACS medicinal chemistry letters2021
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
Article in ACS medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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The trial behind it
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Who cites it
8 citing papers in PubMed.
- Synthesis, Structure, and Antileishmanial Activity of Novel 1,2,4-Trioxolanes, 1,2,4,5-Tetraoxanes and Their Respective Deoxygenated Controls.ChemMedChem · 2026Article
- Three decades of selective product formationRSC advances · 2025Review
- Identifying a next-generation antimalarial trioxolane in a landscape of artemisinin partial resistance.Science advances · 2025Article
- Synthesis and In Vivo Profiling of Desymmetrized Antimalarial Trioxolanes with Diverse Carbamate Side Chains.ACS medicinal chemistry letters · 2024Article
- Diversified Synthesis ofACS omega · 2024Article
- Characterization of antimalarial activity of artemisinin-based hybrid drugs.Antimicrobial agents and chemotherapy · 2024Article
- Artefenomel Regioisomer RLA-3107 Is a Promising Lead for the Discovery of Next-Generation Endoperoxide Antimalarials.ACS medicinal chemistry letters · 2023Article
- Synthesis, Structure and Antileishmanial Evaluation of Endoperoxide-Pyrazole Hybrids.Molecules (Basel, Switzerland) · 2022Article
Corrections and comments
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Authors and funding
12 authors.
Funding
Abstract
Synthetic endoperoxide antimalarials, such as 1,2,4-trioxolanes and 1,2,4,5-tetraoxanes, are promising successors for current front-line antimalarials, semisynthetic artemisinin derivatives. However, limited solubility of second-generation analogues in biological-relevant media represents a barrier in clinical development. We present methodology for the synthesis of nonlinear analogues of second-generation tetraoxane antimalarials E209 and N205 to investigate reduced molecular symmetry on in vitro antimalarial activity and physicochemical properties. While maintaining good antimalarial activity and metabolic stability, head-to-head comparison of linear and nonlinear counterparts showed up to 10-fold improvement in FaSSIF solubility for three of the four analogues studied. Pharmacokinetic studies in rats comparing a selected nonlinear analogue
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Registered trials
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