1429192-49-3Relevant academic research and scientific papers
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
2,3-DIHYDROQUINAZOLIN-4(1 H)-ONE DERIVATIVES FOR USE IN THE TREATMENT OF VIRAL INFECTIONS
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Page/Page column 20; 21; 23, (2014/05/07)
Use of 2,3-dihydroquinazolin-4(lH)-one cyclic derivatives of formula (I) for the treatment of infection with viruses entering cells by endocytosis, especially filovirus such as Ebolavirus.
2,3-dihydroquinazolin-4(1H)-one derivatives for use in the treatment of viral infections
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Page/Page column 0040; 0041, (2014/05/07)
Use of 2,3-dihydroquinazolin-4(1H)-one cyclic derivatives of formula (I) for the treatment of infection with viruses entering cells by endocytosis, especially filovirus such as Ebolavirus
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.
