Synthesis and Preliminary Antiviral Activities of Piperidine-substituted Purines against HIV and Influenza A/H1N1 Infections.

We have developed a series of N²-(1-(substituted-aryl)piperidin-4-yl)-N⁶-mesityl-9 H-purine-2,6-diamine derivatives as potent antiviral agents. Preliminary biological evaluation indicated that nearly half of them possessed remarkable HIV inhibitory potencies in cellular assays. In particular, FZJ 13 appeared to be the most notable one, which displayed anti- HIV-1 activity compared to 3 TC. Moreover, an unexpected finding was that FZJ 05 displayed significant potency against influenza A/H1N1 (strain A/ PR/8/34) in Madin-Darby canine kidney cells with EC₅₀ values much lower than those of ribavirin, amantadine, and rimantadine. The results suggest that these novel purine derivatives have the potential to be further developed as new therapeutic agents against HIV-1 or influenza virus. [ABSTRACT FROM AUTHOR]