Biendl, Stefan published the artcileDiscovery of novel antischistosomal scaffolds from the open access Pandemic Response Box, Product Details of C12H9N3O5S, the main research area is antischistosomal scaffold pandemic response box schistosomiasis praziquantel; Anthelminthics; Pandemic Response Box; Schistosoma mansoni; drug discovery; drug repurposing; schistosomiasis.
BackgroundTreatment and control of schistosomiasis rely on a single drug, praziquantel. New orally active antischistosomals featuring novel mol. scaffolds are urgently needed to prevent the emergence of resistance. MethodsWe screened 400 drug-like compounds contained in the open-access Pandemic Response Box (PRB) against newly transformed schistosomula (NTS) at a concentration of 10 μM scoring death, changes in motility, and morphol. alterations. Compounds displaying an activity ≥66% at 72 h underwent testing against adult Schistosoma mansoni in vitro. Fast-acting (≥66% at 24 h), nontoxic drugs focusing on late-stage and approved drugs were investigated in the patent S. mansoni mouse model. ResultsWe identified 26 hits active against NTS, of which 17 elicited ≥66% activity against adult S. mansoni following 24 h of drug exposure. The highest activity against adult S. mansoni was observed with MMV1581558 (EC50 value of 0.18 ± 0.01 μM) and nitazoxanide (0.47 ± 0.07 μM). Of the five compounds tested in vivo, MMV1581558 and the approved drug ozanimod reduced average worm burden vs. controls by 42 % and 36 %, resp., after a single oral dose of 200 mg/kg bodyweight in mice harboring a chronic S. mansoni infection. ConclusionMMV1581558 discovered from screening the PRB represents a novel antischistosomal scaffold with high in vitro antischistosomal activity amenable to chem. modification for drug development.
Expert Review of Anti-Infective Therapy published new progress about Death. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Product Details of C12H9N3O5S.
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