{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["15(12)"],"submitter":["Hermann T"],"pubmed_abstract":["MMV's Malaria Box compound MMV030666 shows multi-stage activity against various strains of <i>Plasmodium falciparum</i> and lacks resistance development. To evaluate the importance of its diarylether partial structure, diarylthioethers and diphenylamines with varying substitution patterns were prepared. A number of evident structure-activity relationships were revealed. Physicochemical and pharmacokinetic parameters were determined experimentally (passive permeability) or calculated. Compared to the lead compound a diarylthioether was more active and less cytotoxic resulting in an excellent selectivity index of 850. In addition, pharmacokinetic and physicochemical parameters were improved."],"journal":["Pharmaceuticals (Basel, Switzerland)"],"pagination":["1503"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9783227"],"repository":["biostudies-literature"],"pubmed_title":["New Derivatives of the Multi-Stage Active Malaria Box Compound MMV030666 and Their Antiplasmodial Potencies."],"pmcid":["PMC9783227"],"pubmed_authors":["Maser P","Hermann T","Pferschy-Wenzig EM","Seebacher W","Weis R","Wallner R","Dolensky J","Kaiser M"],"additional_accession":[]},"is_claimable":false,"name":"New Derivatives of the Multi-Stage Active Malaria Box Compound MMV030666 and Their Antiplasmodial Potencies.","description":"MMV's Malaria Box compound MMV030666 shows multi-stage activity against various strains of <i>Plasmodium falciparum</i> and lacks resistance development. To evaluate the importance of its diarylether partial structure, diarylthioethers and diphenylamines with varying substitution patterns were prepared. A number of evident structure-activity relationships were revealed. Physicochemical and pharmacokinetic parameters were determined experimentally (passive permeability) or calculated. Compared to the lead compound a diarylthioether was more active and less cytotoxic resulting in an excellent selectivity index of 850. In addition, pharmacokinetic and physicochemical parameters were improved.","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Dec","modification":"2025-04-18T15:59:45.735Z","creation":"2025-04-07T02:53:28.191Z"},"accession":"S-EPMC9783227","cross_references":{"pubmed":["36558954"],"doi":["10.3390/ph15121503"]}}