An article Discovery of Membrane-Bound Pyrophosphatase Inhibitors Derived from an Isoxazole Fragment WOS:000526402700030 published article about TRYPANOSOMA-BRUCEI; PUMPING PYROPHOSPHATASES; ACIDOCALCISOMES; BISPHOSPHONATES; TARGET in [Vidilaseris, Keni; Goldman, Adrian] Univ Helsinki, Div Biochem, Dept Biosci, FI-00014 Helsinki, Finland; [Goldman, Adrian] Univ Leeds, Sch Biomed Sci, Leeds LS2 9JT, W Yorkshire, England; [Goldman, Adrian] Univ Leeds, Astbury Ctr Struct Mol Biol, Leeds LS2 9JT, W Yorkshire, England; [Johansson, Niklas G.; Turku, Ainoleena; Dreano, Loic; Perez, Daniel Ayuso; Zhang, Yuezhou; Tamminen, Matti; Grazhdankin, Evgeni; Kiriazis, Alexandros; af Gennas, Gustav Boije; Xhaard, Henri] Univ Helsinki, Drug Res Program, Div Pharmaceut Chem & Technol, Fac Pharm, FI-00014 Helsinki, Finland; [Khattab, Ayman; Meri, Seppo] Univ Helsinki, Malaria Res Lab, Translat Immunol Res Program, Dept Bacteriol & Immunol,Haartman Inst, FI-00014 Helsinki, Finland; [Wilkinson, Aaron; Fishwick, Colin W. G.] Univ Leeds, Sch Chem, Leeds LS2 9JT, W Yorkshire, England in 2020.0, Cited 34.0. Computed Properties of C8H7NO3. The Name is 1-(4-Nitrophenyl)ethanone. Through research, I have a further understanding and discovery of 100-19-6
Membrane-bound pyrophosphatases (mPPases) regulate energy homeostasis in pathogenic protozoan parasites and lack human homologues, which makes them promising targets in e.g. malaria. Yet only few nonphosphorus inhibitors have been reported so far. Here, we explore an isoxazole fragment hit, leading to the discovery of small mPPase inhibitors with 6-10 mu M IC50 values in the Thermotoga maritima test system. Promisingly, the compounds retained activity against Plasmodium falciparum mPPase in membranes and inhibited parasite growth.
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Benzodioxan,
,1,4-Benzodioxane | C8H8O2 – PubChem