1429192-67-5Relevant 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
N -Methyldihydroquinazolinone derivatives of retro-2 with enhanced efficacy against shiga toxin
Noel, Romain,Gupta, Neetu,Pons, Valérie,Goudet, Amélie,Garcia-Castillo, Maria Daniela,Michau, Aurélien,Martinez, Jennifer,Buisson, David-Alexandre,Johannes, Ludger,Gillet, Daniel,Barbier, Julien,Cintrat, Jean-Christophe
, p. 3404 - 3413 (2013/06/04)
The Retro-2 molecule protects cells against Shiga toxins by specifically blocking retrograde transport from early endosomes to the trans-Golgi network. A SAR study has been carried out to identify more potent compounds. Cyclization and modifications of Retro-2 led to a compound with roughly 100-fold improvement of the EC50 against Shiga toxin cytotoxicity measured in a cell protein synthesis assay. We also demonstrated that only one enantiomer of the dihydroquinazolinone reported herein is bioactive.