Synthesis and Antileishmanial Activity of 1,2,4,5-Tetraoxanes against Leishmania donovani [PDF]
Molecules, 2020 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
Interaction between the Antimalarial Drug Dispiro-Tetraoxanes and Human Serum Albumin: A Combined Study with Spectroscopic Methods and Computational Studies [PDF]
ACS Omega, 2020 Dispiro-tetraoxanes, a class of fully synthetic peroxides which can be used as an antiplasmodial remedy for multiple drug-resistant strains of Plasmodium falciparum, were selected for the interaction study with human serum albumin (HSA). The insight into
Priyanka Yadav +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]
Pharmaceuticals, 2022 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 +7 more sources
Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii and anti-cancer molecules [PDF]
Journal of the Serbian Chemical Society, 2015 New cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains.
Opsenica Dejan M. +6 more
doaj +7 more sources
Identification of Potential Antiviral Inhibitors from Hydroxychloroquine and 1,2,4,5-Tetraoxanes Analogues and Investigation of the Mechanism of Action in SARS-CoV-2. [PDF]
Int J Mol Sci, 2022 This study aimed to identify potential inhibitors and investigate the mechanism of action on SARS-CoV-2 ACE2 receptors using a molecular modeling study and theoretical determination of biological activity. Hydroxychloroquine was used as a pivot structure
Ramos RS +5 more
europepmc +4 more sources
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205. [PDF]
ACS Med Chem Lett, 2021 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.
Woodley CM +11 more
europepmc +4 more sources
Antimalarial, antimycobacterial and antiproliferative activity of phenyl substituted mixed tetraoxanes [PDF]
Journal of the Serbian Chemical Society, 2003 Mixed tetraoxanes of the 4"-phenyl-substituted cyclohexyl-spirotetraoxacyclohexyl- spirocholate series have been prepared and evaluated as possible antimalarials, antiproliferatives and antimycobacterials.
Opsenica Dejan M. +3 more
doaj +8 more sources
Structure-activity relationship study of steroidal 1,2,4,5-tetraoxane animalarials using computational procedures [PDF]
Journal of the Serbian Chemical Society, 2005 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 +9 more sources
Synthesis, Structure and Antileishmanial Evaluation of Endoperoxide–Pyrazole Hybrids [PDF]
Molecules, 2022 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 +6 more sources
Examination of the cytotoxic and embryotoxic potential and underlying mechanisms of next-generation synthetic trioxolane and tetraoxane antimalarials. [PDF]
Mol Med, 2012 Semisynthetic artemisinin-based therapies are the first-line treatment for P. falciparum malaria, but next-generation synthetic drug candidates are urgently required to improve availability and respond to the emergence of artemisinin-resistant parasites.
Copple IM +13 more
europepmc +5 more sources