title: Synthesis and biological evaluation of nucleoside analogues having 6-chloropurine as anti-SARS-CoV agents.
abstract: Nucleoside analogues that have 6-chloropurine as the nucleobase were synthesized and evaluated for anti-SARS-CoV activity by plaque reduction and yield reduction assays in order to develop novel anti-SARS-CoV agents. Among these analogues, two compounds, namely, 1 and 11, exhibited promising anti-SARS-CoV activity that was comparable to those of mizoribine and ribavirin, which are known anti-SARS-CoV agents. Moreover, we observed several SAR trends such as the antiviral effects of the 6-chloropurine moiety, unprotected 5'-hydroxyl group and benzoylated 5'-hydroxyl group.
authors.affiliation: Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University, 1314-1 Shido, Sanuki, Kagawa 769-2193, Japan.
authors.forename: Masahiro
authors.initials: M
authors.lastname: Ikejiri
authors.forename: Masayuki
authors.initials: M
authors.lastname: Saijo
authors.forename: Shigeru
authors.initials: S
authors.lastname: Morikawa
authors.forename: Shuetsu
authors.initials: S
authors.lastname: Fukushi
authors.forename: Tetsuya
authors.initials: T
authors.lastname: Mizutani
authors.forename: Ichiro
authors.initials: I
authors.lastname: Kurane
authors.forename: Tokumi
authors.initials: T
authors.lastname: Maruyama
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005069:Evaluation Studies as Topic; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D008968:Molecular Conformation; D009705:Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology*; D011687:Purines / Q000737:chemistry*; D045473:Severe acute respiratory syndrome-related coronavirus / Q000378:metabolism*; D045169:Severe Acute Respiratory Syndrome / Q000188:drug therapy*; D014709:Vero Cells
chemical_list: D000998:Antiviral Agents; D009705:Nucleosides; D011687:Purines; C079308:6-chloropurine