21567-55-5Relevant academic research and scientific papers
FERROPTOSIS INHIBITORS–DIARYLAMINE PARA-ACETAMIDES
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, (2021/09/11)
Provided are compounds that inhibit ferroptosis activity, or modulate or inhibit a disease associated with ferroptosis dysregulation, such as neuropathy, ischemia reperfusion injury, acute kidney failure and cancer, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice
Gujjar, Ramesh,El Mazouni, Farah,White, Karen L.,White, John,Creason, Sharon,Shackleford, David M.,Deng, Xiaoyi,Charman, William N.,Bathurst, Ian,Burrows, Jeremy,Floyd, David M.,Matthews, David,Buckner, Frederick S.,Charman, Susan A.,Phillips, Margaret A.,Rathod, Pradipsinh K.
, p. 3935 - 3949 (2011/07/31)
Malaria is one of the leading causes of severe infectious disease worldwide; yet, our ability to maintain effective therapy to combat the illness is continually challenged by the emergence of drug resistance.We previously reported identification of a new class of triazolopyrimidine-based Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors with antimalarial activity, leading to the discovery of a new lead series and novel target for drug development. Active compounds from the series contained a triazolopyrimidine ring attached to an aromatic group through a bridging nitrogen atom. Herein, we describe systematic efforts to optimize the aromatic functionality with the goal of improving potency and in vivo properties of compounds from the series. These studies led to the identification of two new substituted aniline moieties (4-SF5-Ph and 3,5-Di-F-4- CF 3-Ph), which, when coupled to the triazolopyrimidine ring, showed good plasma exposure and better efficacy in the Plasmodium berghei mouse model of the disease than previously reported compounds from the series.
Imino- and bis-imino-pyridines with N-ter-butyl-N-aminoxyl group: Synthesis, oxidation and use as ligand towards M2+ (Mn, Ni, Zn) and Gd3+
Uerpmann, Carsten,Henner, Bernard J.L.,Guérin, Christian,Carré, Fran?is
, p. 197 - 210 (2007/10/03)
Imino- and bis-iminopyridine ligands bearing N-ter-butylhydroxy groups were synthesized by the condensation reaction between a N-ter-butylhydroxy substituted aniline and 2-formylpyridine, 2-acetylpyridine and 2,6-bis-acetylpyridine. The N-ter-butylaminoxy radicals obtained after oxidation using PbO2 or Ag2O were studied by EPR spectroscopy in solution. Indeed, complete decomposition was observed during isolation of these radical derivatives. The N-ter-butylhydroxy substituted ligands obtained were complexed with Mn2+, Ni2+, Zn2+ and Gd 3+ salts; the obtained complexes were characterized and oxidized to give the aminoxy analogs, which were studied using IR, UV and EPR spectroscopies.
