Synthesis and in vitro activity of 4' and 5'-modified analogues of apiosyl nucleosides as potent anti-HCV agents.
Novel doubly branched apio dideoxynucleosides were synthesized starting from 1,3-dihydroxyacetone using an ozonolysis and Grignard addition as key steps, and evaluated for anti-hepatitis C virus (HCV) activity. The adenine derivative 24 showed significant anti-HCV activity, indicating that the branches at the 4',5'-position of the apiosyl ring led to favorable interaction with HCV polymerase.
Li
Hua
H
BK21-Project Team, College of Pharmacy, Chosun University, Kwangju, Republic of Korea.
Lee
Wonjae
W
Hong
Joon Hee
JH
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015224:Dideoxynucleosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D016174:Hepacivirus / Q000187:drug effects*; D006801:Humans; D015394:Molecular Structure; D010429:Pentoses / Q000737:chemistry*
D000998:Antiviral Agents; D015224:Dideoxynucleosides; D010429:Pentoses; C004983:apiose