The Experts below are selected from a list of 48 Experts worldwide ranked by ideXlab platform
David Standring - One of the best experts on this subject based on the ideXlab platform.
-
Synthesis and Pharmacokinetics of Valopicitabine (NM283), an Efficient Prodrug of the Potent Anti-HCV Agent 2‘-C-Methylcytidine
Journal of medicinal chemistry, 2006Co-Authors: Claire Pierra, Agnes Amador, Samira Benzaria, Steven Mathieu, Adel M Moussa, Edward G Bridges, Erika Cretton-scott, Marc D'amours, John Mao, David StandringAbstract:In our search for new therapeutic agents against chronic hepatitis C, a ribonucleoside analogue, 2'-C-methylcytidine, was discovered to be a potent and selective inhibitor in cell culture of a number of RNA viruses, including the pestivirus bovine viral diarrhea virus, a surrogate model for hepatitis C virus (HCV), and three flaviviruses, namely, yellow fever virus, West Nile virus, and dengue-2 virus. However, pharmacokinetic studies revealed that 2'-C-methylcytidine suffers from a low oral bioavailability. To overcome this limitation, we have synthesized the 3'-O-l-valinyl ester derivative (dihydrochloride form, Valopicitabine, NM283) of 2'-C-methylcytidine. We detail herein for the first time the chemical synthesis and physicochemical characteristics of this anti-HCV prodrug candidate, as well as a comparative study of its pharmacokinetic parameters with those of its parent nucleoside analogue, 2'-C-methylcytidine.
-
synthesis and pharmacokinetics of Valopicitabine nm283 an efficient prodrug of the potent anti hcv agent 2 c methylcytidine
Journal of Medicinal Chemistry, 2006Co-Authors: Claire Pierra, Agnes Amador, Samira Benzaria, Erika Crettonscott, Marc Damours, Steven Mathieu, Adel M Moussa, Edward G Bridges, David Standring, Jeanpierre SommadossiAbstract:In our search for new therapeutic agents against chronic hepatitis C, a ribonucleoside analogue, 2‘-C-methylcytidine, was discovered to be a potent and selective inhibitor in cell culture of a number of RNA viruses, including the pestivirus bovine viral diarrhea virus, a surrogate model for hepatitis C virus (HCV), and three flaviviruses, namely, yellow fever virus, West Nile virus, and dengue-2 virus. However, pharmacokinetic studies revealed that 2‘-C-methylcytidine suffers from a low oral bioavailability. To overcome this limitation, we have synthesized the 3‘-O-l-valinyl ester derivative (dihydrochloride form, Valopicitabine, NM283) of 2‘-C-methylcytidine. We detail herein for the first time the chemical synthesis and physicochemical characteristics of this anti-HCV prodrug candidate, as well as a comparative study of its pharmacokinetic parameters with those of its parent nucleoside analogue, 2‘-C-methylcytidine.
Claire Pierra - One of the best experts on this subject based on the ideXlab platform.
-
Synthesis and Pharmacokinetics of Valopicitabine (NM283), an Efficient Prodrug of the Potent Anti-HCV Agent 2‘-C-Methylcytidine
Journal of medicinal chemistry, 2006Co-Authors: Claire Pierra, Agnes Amador, Samira Benzaria, Steven Mathieu, Adel M Moussa, Edward G Bridges, Erika Cretton-scott, Marc D'amours, John Mao, David StandringAbstract:In our search for new therapeutic agents against chronic hepatitis C, a ribonucleoside analogue, 2'-C-methylcytidine, was discovered to be a potent and selective inhibitor in cell culture of a number of RNA viruses, including the pestivirus bovine viral diarrhea virus, a surrogate model for hepatitis C virus (HCV), and three flaviviruses, namely, yellow fever virus, West Nile virus, and dengue-2 virus. However, pharmacokinetic studies revealed that 2'-C-methylcytidine suffers from a low oral bioavailability. To overcome this limitation, we have synthesized the 3'-O-l-valinyl ester derivative (dihydrochloride form, Valopicitabine, NM283) of 2'-C-methylcytidine. We detail herein for the first time the chemical synthesis and physicochemical characteristics of this anti-HCV prodrug candidate, as well as a comparative study of its pharmacokinetic parameters with those of its parent nucleoside analogue, 2'-C-methylcytidine.
-
synthesis and pharmacokinetics of Valopicitabine nm283 an efficient prodrug of the potent anti hcv agent 2 c methylcytidine
Journal of Medicinal Chemistry, 2006Co-Authors: Claire Pierra, Agnes Amador, Samira Benzaria, Erika Crettonscott, Marc Damours, Steven Mathieu, Adel M Moussa, Edward G Bridges, David Standring, Jeanpierre SommadossiAbstract:In our search for new therapeutic agents against chronic hepatitis C, a ribonucleoside analogue, 2‘-C-methylcytidine, was discovered to be a potent and selective inhibitor in cell culture of a number of RNA viruses, including the pestivirus bovine viral diarrhea virus, a surrogate model for hepatitis C virus (HCV), and three flaviviruses, namely, yellow fever virus, West Nile virus, and dengue-2 virus. However, pharmacokinetic studies revealed that 2‘-C-methylcytidine suffers from a low oral bioavailability. To overcome this limitation, we have synthesized the 3‘-O-l-valinyl ester derivative (dihydrochloride form, Valopicitabine, NM283) of 2‘-C-methylcytidine. We detail herein for the first time the chemical synthesis and physicochemical characteristics of this anti-HCV prodrug candidate, as well as a comparative study of its pharmacokinetic parameters with those of its parent nucleoside analogue, 2‘-C-methylcytidine.
Johan Neyts - One of the best experts on this subject based on the ideXlab platform.
-
ribavirin antagonizes the in vitro anti hepatitis c virus activity of 2 c methylcytidine the active component of Valopicitabine
Antimicrobial Agents and Chemotherapy, 2006Co-Authors: Lotte Coelmont, Jan Paeshuyse, Marc P. Windisch, Erik De Clercq, Ralf Bartenschlager, Johan NeytsAbstract:Ribavirin antagonizes the in vitro anti-hepatitis C virus (HCV) activity of the pyrimidine nucleoside analogue 2′-C-methylcytidine, the active component of the experimental anti-HCV drug Valopicitabine. In contrast, the combination of ribavirin with either the purine nucleoside analogue 2′-C-methyladenosine or the HCV protease inhibitor VX-950 resulted in an additive antiviral activity. These findings may have implications when planning clinical studies with Valopicitabine.
-
Ribavirin Antagonizes the In Vitro Anti-Hepatitis C Virus Activity of 2′-C-Methylcytidine, the Active Component of Valopicitabine
Antimicrobial agents and chemotherapy, 2006Co-Authors: Lotte Coelmont, Jan Paeshuyse, Marc P. Windisch, Erik De Clercq, Ralf Bartenschlager, Johan NeytsAbstract:Ribavirin antagonizes the in vitro anti-hepatitis C virus (HCV) activity of the pyrimidine nucleoside analogue 2′-C-methylcytidine, the active component of the experimental anti-HCV drug Valopicitabine. In contrast, the combination of ribavirin with either the purine nucleoside analogue 2′-C-methyladenosine or the HCV protease inhibitor VX-950 resulted in an additive antiviral activity. These findings may have implications when planning clinical studies with Valopicitabine.
Jeanpierre Sommadossi - One of the best experts on this subject based on the ideXlab platform.
-
synthesis and pharmacokinetics of Valopicitabine nm283 an efficient prodrug of the potent anti hcv agent 2 c methylcytidine
Journal of Medicinal Chemistry, 2006Co-Authors: Claire Pierra, Agnes Amador, Samira Benzaria, Erika Crettonscott, Marc Damours, Steven Mathieu, Adel M Moussa, Edward G Bridges, David Standring, Jeanpierre SommadossiAbstract:In our search for new therapeutic agents against chronic hepatitis C, a ribonucleoside analogue, 2‘-C-methylcytidine, was discovered to be a potent and selective inhibitor in cell culture of a number of RNA viruses, including the pestivirus bovine viral diarrhea virus, a surrogate model for hepatitis C virus (HCV), and three flaviviruses, namely, yellow fever virus, West Nile virus, and dengue-2 virus. However, pharmacokinetic studies revealed that 2‘-C-methylcytidine suffers from a low oral bioavailability. To overcome this limitation, we have synthesized the 3‘-O-l-valinyl ester derivative (dihydrochloride form, Valopicitabine, NM283) of 2‘-C-methylcytidine. We detail herein for the first time the chemical synthesis and physicochemical characteristics of this anti-HCV prodrug candidate, as well as a comparative study of its pharmacokinetic parameters with those of its parent nucleoside analogue, 2‘-C-methylcytidine.
Agnes Amador - One of the best experts on this subject based on the ideXlab platform.
-
Synthesis and Pharmacokinetics of Valopicitabine (NM283), an Efficient Prodrug of the Potent Anti-HCV Agent 2‘-C-Methylcytidine
Journal of medicinal chemistry, 2006Co-Authors: Claire Pierra, Agnes Amador, Samira Benzaria, Steven Mathieu, Adel M Moussa, Edward G Bridges, Erika Cretton-scott, Marc D'amours, John Mao, David StandringAbstract:In our search for new therapeutic agents against chronic hepatitis C, a ribonucleoside analogue, 2'-C-methylcytidine, was discovered to be a potent and selective inhibitor in cell culture of a number of RNA viruses, including the pestivirus bovine viral diarrhea virus, a surrogate model for hepatitis C virus (HCV), and three flaviviruses, namely, yellow fever virus, West Nile virus, and dengue-2 virus. However, pharmacokinetic studies revealed that 2'-C-methylcytidine suffers from a low oral bioavailability. To overcome this limitation, we have synthesized the 3'-O-l-valinyl ester derivative (dihydrochloride form, Valopicitabine, NM283) of 2'-C-methylcytidine. We detail herein for the first time the chemical synthesis and physicochemical characteristics of this anti-HCV prodrug candidate, as well as a comparative study of its pharmacokinetic parameters with those of its parent nucleoside analogue, 2'-C-methylcytidine.
-
synthesis and pharmacokinetics of Valopicitabine nm283 an efficient prodrug of the potent anti hcv agent 2 c methylcytidine
Journal of Medicinal Chemistry, 2006Co-Authors: Claire Pierra, Agnes Amador, Samira Benzaria, Erika Crettonscott, Marc Damours, Steven Mathieu, Adel M Moussa, Edward G Bridges, David Standring, Jeanpierre SommadossiAbstract:In our search for new therapeutic agents against chronic hepatitis C, a ribonucleoside analogue, 2‘-C-methylcytidine, was discovered to be a potent and selective inhibitor in cell culture of a number of RNA viruses, including the pestivirus bovine viral diarrhea virus, a surrogate model for hepatitis C virus (HCV), and three flaviviruses, namely, yellow fever virus, West Nile virus, and dengue-2 virus. However, pharmacokinetic studies revealed that 2‘-C-methylcytidine suffers from a low oral bioavailability. To overcome this limitation, we have synthesized the 3‘-O-l-valinyl ester derivative (dihydrochloride form, Valopicitabine, NM283) of 2‘-C-methylcytidine. We detail herein for the first time the chemical synthesis and physicochemical characteristics of this anti-HCV prodrug candidate, as well as a comparative study of its pharmacokinetic parameters with those of its parent nucleoside analogue, 2‘-C-methylcytidine.
