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
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 +4 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
Unlocking the antimalarial potential of novel steroid-tetraoxane hybrids through consensus molecular docking and molecular dynamics investigation [PDF]
The emergence of Plasmodium falciparum resistance to artemisinin-based combination therapies necessitates the development of novel antimalarial agents.
Dipankar Nath +4 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
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
Synthesis and in vitro Study of Artemisinin/Synthetic Peroxide-Based Hybrid Compounds against SARS-CoV-2 and Cancer. [PDF]
Hybrid power: New artemisinin‐ and synthetic peroxide‐based hybrids, highly active in vitro against leukemia cell lines and SARS‐CoV‐2, were synthesized. Remarkably, the most active anti‐cancer hybrid compounds are also the most potent and selective against SARS‐CoV‐2. Abstract The newly emerged severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐
Herrmann L +13 more
europepmc +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
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
Diversified Synthesis of N‑Benzoyl Piperidine Tetraoxane Analogues Using Molybdenum Trioxide as a Newer Catalyst and Its Antiplasmodial Activity [PDF]
Arvind Kumar +4 more
doaj +4 more sources

