1616809-39-2Relevant articles and documents
Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector
Sari, Ozkan,Boucle, Sebastien,Cox, Bryan D.,Ozturk, Tugba,Russell, Olivia Ollinger,Bassit, Leda,Amblard, Franck,Schinazi, Raymond F.
, p. 407 - 421 (2017/07/10)
The synthesis of novel series of sulfamoylbenzamides as HBV capsid assembly effector is reported. The structure was divided into five parts which were independently modified as part of our lead optimization. All synthesized compounds were evaluated for their anti-HBV activity and toxicity in human hepatocytes, lymphocytes and other cells. Additionally, we assessed their effect on HBV cccDNA formation in an HBeAg reporter cell-based assay. Among the 27 compounds reported, several analogs exhibited submicromolar activities and significant reduction of HBeAg secretion. Selected compounds were studied under negative-stain electron microscopy for their ability to disrupt the HBV capsid formation. Structures were modeled into a binding site recently identified in the HBV capsid protein for similar molecules to rationalize the structure-activity relationships for this family of compounds.
NOVEL ANTIVIRAL AGENTS AGAINST HBV INFECTION
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Paragraph 0472; 0473; 0474, (2014/07/21)
The present invention is directed toward novel compounds and novel methods of use of said compounds of the formula (I), useful as nucleocapsid assembly inhibitors for the treatment of viruses, especially but not exclusively, including pregenomic RNA encapsidation inhibitors of HBV for the treatment of Hepatitis B virus (HBV) infection and related conditions. (Formula (I)) Including hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein A, R1, R2, R3, R4, R5, R6, R7, and R8 are defined herein.