Lv, Kai published the artcileDesign, synthesis and anti-HBV activity of NVR3-778 derivatives, Application In Synthesis of 73874-95-0, the main research area is preparation antiviral hepatitis B HBV NVR3 778 derivative; Anti-HBV activity; Capsid assembly modulators; NVR3-778; Structure modification; Sulfamoylbenzamides.
NVR3-778, one of the most advanced capsid assembly modulators (CAMs), is currently in phase II clin. trial for the treatment of HBV infection. In this study, we reported the first structure optimization of NVR3-778. Compound 2d was found to exhibit more potent anti-HBV activity (IC50: 0.25μM), lower cytotoxicity (CC50: 10.68μM) and higher selectivity index (SI: 40.72) than NVR3-778 (IC50: 0.33μM; CC50: 5.14μM; SI: 18.36) in vitro, and also display similar inhibitory effect on the assembly of HBV capsids as NVR3-778. Mol. docking further suggested that compound 2d might form a stronger interaction with core protein. Moreover, compound 2d also showed acceptable pharmacokinetic profiles. Currently compound 2d was selected as a new lead for further modifications, and studies to determine the in vivo anti-HBV studies of 2d will begin soon.
Bioorganic Chemistry published new progress about Antiviral agents. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Application In Synthesis of 73874-95-0.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem