hbf-0259 has been researched along with Hepatitis-B* in 2 studies
1 review(s) available for hbf-0259 and Hepatitis-B
| Article | Year |
|---|---|
A review of non-nucleoside anti-hepatitis B virus agents.
Hepatitis B Virus is the most common cause of chronic liver disease worldwide. Currently approved agents of chronic HBV infection treatment include interferon and nucleoside analogues. However, the side effects of interferon and the viral resistance of nucleoside analogues make the current treatment far from satisfactory. Therefore, new drugs with novel structures and mechanisms are needed. Recently, a number of non-nucleoside HBV inhibitors have been obtained from natural sources or prepared by synthesis/semi-synthesis. Some of them exhibited potent anti-HBV activity with novel mechanisms. These compounds provide useful information for the medicinal chemist to develop novel non-nucleoside compounds as anti-HBV agents. Topics: Animals; Antiviral Agents; Biological Products; Hepatitis B; Hepatitis B virus; Humans; Small Molecule Libraries | 2014 |
1 other study(ies) available for hbf-0259 and Hepatitis-B
| Article | Year |
|---|---|
Design, synthesis, and biological evaluation of triazolo-pyrimidine derivatives as novel inhibitors of hepatitis B virus surface antigen (HBsAg) secretion.
The high levels of hepatitis B virus (HBV) surface antigen (HBsAg)-bearing subviral particles in the serum of chronically infected individuals play an important role in suppressing HBV-specific immune response and are only mildly affected by the current small molecule therapies. Thus, a therapy that specifically reduces HBsAg serum levels could be used in combination therapy with nucleos(t)ide drugs or permit therapeutic vaccination for the treatment of HBV infection. Herein, we report the design, synthesis, and evaluation of novel triazolo-pyrimidine inhibitors (1, 3, and 4) of HBsAg cellular secretion, with activity against drug-resistant HBV variants. Extensive SAR led to substantial improvements in the EC(50) of the parent compound, 5 (HBF-0259), with the best being 3c, with EC(50) = 1.4 ± 0.4 μM, SI ≥ 36. The lead candidates, both 1a (PBHBV-001) and 3c (PBHBV-2-15), were well-tolerated in both normal and HBV-transgenic mice and exhibited acceptable pharmacokinetics and bioavailability in Sprague-Dawley rats. Topics: Adenine; Animals; Antiviral Agents; Biological Availability; Drug Design; Drug Resistance, Viral; Guanine; Hep G2 Cells; Hepatitis B; Hepatitis B Surface Antigens; Hepatitis B virus; Humans; Lamivudine; Male; Mice; Models, Chemical; Molecular Structure; Mutation; Organophosphonates; Pyrimidines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Tenofovir; Tetrazoles | 2011 |