title: Synthesis, physicochemical and pharmacokinetic studies of potential prodrugs of beta-L-2'-deoxycytidine, a selective and specific anti-HBV agent.
abstract: beta-L-2'-Deoxycytidine (beta-L-dC) is a potent, selective and specific anti-hepatitis B virus (HBV) agent. To improve its oral bioavailability, several derivatives involving sugar or base acylation, as well N4-derivatization with an N,N-(dimethylamino)methylene function, were synthesized. The physicochemical characteristics (including chemical stabilities, solubilities and distribution coefficient values) and pharmacokinetics of these compounds were determined and compared with those of the parent drug, beta-L-dC.
authors.affiliation: Laboratoire Coopératif Idenix-CNRS-Université Montpellier II, Montpellier, France.
authors.forename: Claire
authors.initials: C
authors.lastname: Pierra
authors.forename: Samira
authors.initials: S
authors.lastname: Benzaria
authors.forename: David
authors.initials: D
authors.lastname: Dukhan
authors.forename: Anna Giulia
authors.initials: AG
authors.lastname: Loi
authors.forename: Paolo
authors.initials: P
authors.lastname: La Colla
authors.forename: Edward
authors.initials: E
authors.lastname: Bridges
authors.forename: John
authors.initials: J
authors.lastname: Mao
authors.forename: David
authors.initials: D
authors.lastname: Standring
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Sommadossi
authors.forename: Gilles
authors.initials: G
authors.lastname: Gosselin
mesh_terms: D000215:Acylation; D000284:Administration, Oral; D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D003841:Deoxycytidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000882:Haplorhini; D006515:Hepatitis B virus / Q000187:drug effects* / Q000378:metabolism; D008826:Microbial Sensitivity Tests; D011355:Prodrugs / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D012995:Solubility
chemical_list: D000998:Antiviral Agents; D011355:Prodrugs; C479246:monoval-2'-deoxy-beta-L-cytidine; D003841:Deoxycytidine