1510796-70-9Relevant academic research and scientific papers
(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.
