5-Phenoxy Primaquine Analogs and the Tetraoxane Hybrid as Antimalarial Agents [PDF]
The rapid emergence of drug resistance to the current antimalarial agents has led to the urgent need for the discovery of new and effective compounds.
Somruedee Jansongsaeng+4 more
doaj +8 more sources
Synthesis and Antileishmanial Activity of 1,2,4,5-Tetraoxanes against Leishmania donovani [PDF]
A chemically diverse range of novel tetraoxanes was synthesized and evaluated in vitro against intramacrophage amastigote forms of Leishmania donovani. All 15 tested tetraoxanes displayed activity, with IC50 values ranging from 2 to 45 µm.
Lília I. L. Cabral+5 more
doaj +8 more sources
Antimalarial peroxides: the first intramolecular 1,2,4,5-tetraoxane [PDF]
An intramolecular steroidal 1,2,4,5-tetraoxane has been synthesised in six steps starting from methyl 3-oxo-7a,12a-diacetoxy-5b-cholan-24-oate. The synthesised 1,2,4,5-tetraoxane has moderate in vitro antimalarial activity against P.
BOGDAN A. SOLAJA+3 more
doaj +9 more sources
1,2,4-Trioxolane and 1,2,4,5-Tetraoxane Endoperoxides against Old-World Leishmania Parasites: In Vitro Activity and Mode of Action [PDF]
Leishmaniasis remains one of the ten Neglected Tropical Diseases with significant morbidity and mortality in humans. Current treatment of visceral leishmaniasis is difficult due to a lack of effective, non-toxic, and non-extensive medications. This study
Andreia Mendes+6 more
doaj +4 more sources
A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance [PDF]
Artemisinin-resistantPlasmodium is an increasing problem. Here, using a medicinal chemistry programme, the authors identify a tetraoxane-based drug candidate that shows no cross-resistance with an artemisinin-resistant strain (PfK13-C580Y) and is ...
Paul M. O’Neill+47 more
doaj +4 more sources
Diversified Synthesis of N‑Benzoyl Piperidine Tetraoxane Analogues Using Molybdenum Trioxide as a Newer Catalyst and Its Antiplasmodial Activity [PDF]
Arvind Kumar+4 more
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Synthesis, Structure and Antileishmanial Evaluation of Endoperoxide–Pyrazole Hybrids [PDF]
Leishmaniases are among the most impacting neglected tropical diseases. In attempts to repurpose antimalarial drugs or candidates, it was found that selected 1,2,4-trioxanes, 1,2,4,5-tetraoxanes, and pyrazole-containing chemotypes demonstrated activity ...
Patrícia S. M. Amado+5 more
doaj +2 more sources
Structure-activity relationship study of steroidal 1,2,4,5-tetraoxane animalarials using computational procedures [PDF]
A three-dimensional QSAR pharmacophore model for antimalarial activity of steroidal 1,2,4,5-tetraoxanes was developed from a set of 17 substituted antimalarial derivatives out of 27 analogues that exhibited remarkable in vitro activity (below 100 ng/mL ...
Bhattacharjee Apurba K.+3 more
doaj +5 more sources
In silico modeling of tetraoxane-8-aminoquinoline hybrids active against Plasmodium falciparum [PDF]
Background Quantitative structure-activity relationships (QSAR) is a technique that is used to produce a model that connects biological activities of compounds to their chemical structures, and molecular docking is a technique that reveals the binding ...
Aliyu Wappah Mahmud+2 more
doaj +2 more sources
Cyclic Synthetic Peroxides Inhibit Growth of Entomopathogenic Fungus Ascosphaera apis without Toxic Effect on Bumblebees [PDF]
In recent years, the number of pollinators in the world has significantly decreased. A possible reason for this is the toxic effects of agrochemicals reducing the immunity of insects that leads to their increased susceptibility to pathogens.
Ivan A. Yaremenko+6 more
doaj +2 more sources