1510796-66-3Relevant articles and documents
NEW COMPOUNDS HAVING A PROTECTIVE ACTIVITY AGAINST TOXINS WITH INTRACELLULAR ACTIVITY
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Paragraph 0095, (2015/11/18)
The present invention concerns a new family of 2,3-dihydroquinazolin-4(1H)-one compounds of general formula (I), and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as ricin or Shiga toxin, for example, using
(S)-N-methyldihydroquinazolinones are the active enantiomers of retro-2 derived compounds against toxins
Gupta, Neetu,Pons, Valerie,Noel, Romain,Buisson, David-Alexandre,Michau, Aurelien,Johannes, Ludger,Gillet, Daniel,Barbier, Julien,Cintrat, Jean-Christophe
, p. 94 - 97 (2014/02/14)
This study reports the synthesis, chromatographic separation, and pharmacological evaluation of the two enantiomers of a new compound, named Retro-2.1, active against toxins by inhibiting intracellular trafficking via the retrograde route. The absolute configuration of the bioactive enantiomer has been assigned from X-ray diffraction to the (S)-enantiomer. To date, (S)-Retro-2.1 is the most potent molecule to counteract the cytotoxic potential of ricin and Shiga toxin, with EC50 values of 23 and 54 nM, respectively.