Synonyms:1,2,4,5-Tetroxane;1,2,4,5-tetraoxane;291-15-6;CHEMBL2071269;DTXSID10467807
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The research presents the synthesis and evaluation of new cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea-based groups for their potential as antimalarial agents against chloroquine-resistant and susceptible Plasmodium falciparum strains, and as anti-cancer molecules. The study involved the synthesis of derivatives using reactants such as gem-dihydroperoxide, benzyl 4-oxocyclohexanecarboxylate, and various coupling agents, followed by comprehensive analyses including NMR, IR, MS, and HPLC to characterize the compounds. The antimalarial activity was assessed using the Malaria SYBR Green I based fluorescence assay against different P. falciparum strains, while cytotoxicity was determined on human normal peripheral blood mononuclear cells (PBMC). Additionally, select compounds were tested for in vitro cytotoxic activity against various human cancer cell lines and in vivo activity against Toxoplasma gondii in a murine model. The experiments utilized techniques like MTT tests for cell survival, flow cytometry for cell cycle analysis, and microscopic examination for morphological assessment of cell death. The study identified derivative 24 as the most promising candidate with low nanomolar antimalarial activities, high selectivity indices, and significant in vivo potential against T. gondii.
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