Synthesis and Antiviral Evaluation of (-)-3′-Methylcarbovir, (-)-3′-Methylabacavir, and Modified Purine Analogues

Autor: Erik De Clercq, Honoré Monti, Christophe Pannecouque, Paul Brémond, Gérard Audran
Rok vydání: 2008
Předmět:
Zdroj: Synthesis. 2009:290-296
ISSN: 1437-210X
0039-7881
DOI: 10.1055/s-0028-1083213
Popis: Starting from ethyl (1 S,4 R)-4-hydroxy-2-methylcyclopent-2-ene-1-carboxylate,as a common enantiopure building block readily obtained by enzymatickinetic resolution of the corresponding racemic derivative, 3′-methylcarbovir,3′-methylabacavir, and three modified analogues were synthesizedvia the linear construction of the purine heterocycles. These derivativeswere evaluated as potential agents against HIV-1, HIV-2, and otherimportant viral pathogens. None of the new compounds had significantantiviral activity at a concentration of 100 μg˙mL -¹ ,which was the highest concentration tested.
Databáze: OpenAIRE