A FACILE SYNTHESIS OF (5-HYDROXY-4-OXO-4H-PYRAN-2-YL)METHYL CARBOXYLATES AND THEIR ANTIVIRAL ACTIVITY AGAINST HEPATITIS C VIRUS

Heterocycles ◽  
2013 ◽  
Vol 87 (6) ◽  
pp. 1349 ◽  
Author(s):  
Tetsuro Shimo ◽  
Yuki Taketsugu ◽  
Takuya Goto ◽  
Masaaki Toyama ◽  
Kohji Yoshimura ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Antiviral Activity ◽  
Facile Synthesis

ChemInform Abstract: A Facile Synthesis of (5-Hydroxy-4-oxo-4H-pyran-2-yl)methyl Carboxylates and Their Antiviral Activity Against Hepatitis C Virus.

ChemInform ◽  
2013 ◽  
Vol 44 (39) ◽  
pp. no-no
Author(s):  
Tetsuro Shimo ◽  
Yuki Taketsugu ◽  
Takuya Goto ◽  
Masaaki Toyama ◽  
Kohji Yoshimura ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Antiviral Activity ◽  
Facile Synthesis

scholarly journals Iron Regulator Hepcidin Exhibits Antiviral Activity against Hepatitis C Virus

PLoS ONE ◽  
2012 ◽  
Vol 7 (10) ◽  
pp. e46631 ◽  
Author(s):  
Hongyan Liu ◽  
Thu Le Trinh ◽  
Huijia Dong ◽  
Robertson Keith ◽  
David Nelson ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Antiviral Activity

scholarly journals Impaired antiviral activity of interferon alpha against hepatitis C virus 2a in Huh-7 cells with a defective Jak-Stat pathway

2010 ◽  
Vol 7 (1) ◽  
pp. 36 ◽  
Author(s):  
Sidhartha Hazari ◽  
Partha K Chandra ◽  
Bret Poat ◽  
Sibnarayan Datta ◽  
Robert F Garry ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Antiviral Activity ◽  
Interferon Alpha ◽  
Stat Pathway

scholarly journals Short-Term Monotherapy with IDX184, a Liver-Targeted Nucleotide Polymerase Inhibitor, in Patients with Chronic Hepatitis C Virus Infection

2012 ◽  
Vol 56 (12) ◽  
pp. 6372-6378 ◽  
Author(s):  
Jacob Lalezari ◽  
David Asmuth ◽  
Arnaldo Casiró ◽  
Hugo Vargas ◽  
Shannon Lawrence ◽  
...  
Keyword(s):  
Chronic Hepatitis ◽  
Hepatitis C Virus ◽  
Viral Load ◽  
Hepatitis C ◽  
Adverse Events ◽  
Antiviral Activity ◽  
Chronic Hepatitis C ◽  
Hcv Rna ◽  
Plasma Exposure ◽  
Chronic Hepatitis C Virus

ABSTRACTIDX184 is a liver-targeted prodrug of 2′-methylguanosine (2′-MeG) monophosphate. This study investigated the safety, tolerability, antiviral activity, and pharmacokinetics of IDX184 as a single agent in treatment-naïve patients with genotype-1 chronic hepatitis C virus (HCV) infection. Forty-one patients with baseline HCV RNA ≥ 5 log10IU/ml, alanine aminotransferase (ALT) ≤ 2.5× the upper limit of normal, and compensated liver disease were dosed. Sequential cohorts of 10 patients, randomized 8:2 (active:placebo), received 25, 50, 75, and 100 mg of IDX184 once daily for 3 days, with a 14-day follow-up. There were no safety-related treatment discontinuations or serious adverse events. The adverse events and laboratory abnormalities observed for IDX184- and placebo-treated patients were similar. At the end of the 3-day treatment period, changes from baseline in HCV RNA levels (means ± standard deviations) were −0.5 ± 0.6, −0.7 ± 0.2, −0.6 ± 0.3, and −0.7 ± 0.5 log10for the 25-, 50-, 75-, and 100-mg doses, respectively, while viral load remained unchanged for the pooled placebo patients (−0.05 ± 0.3 log10). Patients with genotype-1a and patients with genotype-1b responded similarly. Serum ALT levels decreased, especially at daily doses ≥ 75 mg. During the posttreatment period, plasma viremia and serum aminotransferase levels returned to near pretreatment levels. No resistance mutations associated with IDX184 were detected. Plasma exposure of IDX184 and its nucleoside metabolite 2′-MeG was dose related and low. Changes in plasma viral load correlated with plasma exposure of 2′-MeG. In conclusion, the results from this proof-of-concept study show that small doses of the liver-targeted prodrug IDX184 were able to deliver significant antiviral activity and support further clinical evaluation of the drug candidate.

The Safety and Antiviral Activity of BZF961 with or without Ritonavir in Patients Infected with Hepatitis C Virus: A Randomized, Multicenter Trial

2018 ◽  
Vol 40 (9) ◽  
pp. 1567-1581.e4
Author(s):  
Eric Lawitz ◽  
Mohamed Bidair ◽  
Thomas Marbury ◽  
Christopher T. Jones ◽  
Avantika Barve ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Antiviral Activity ◽  
Multicenter Trial

Modeling the antiviral activity of ribavirin against hepatitis C virus in cell culture

Hepatology ◽  
2013 ◽  
Vol 58 (4) ◽  
pp. 1203-1206
Author(s):  
Daniel J. Felmlee ◽  
Fei Xiao ◽  
Thomas F. Baumert
Keyword(s):  
Cell Culture ◽  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Antiviral Activity
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