Modifications in the piperazine ring of nucleozin affects anti-influenza activity

ABSTRACT The infection caused by influenza virus is a latent tret, to contribute on the advancement of the discovery and design of nucleozin analogs, a molecule with antiinfluenza activity, we analyzed nucleozin analogs with modifications in the piperazine system, which leads to molecules with larger conformational freedom. Following a new nucleozin synthetic strategy, we obtained three new nucleozin analogs, and two of them were biologically evaluated in vitro and were less active than nucleozin. The loss of activity in the more flexible molecules highlights the need for the piperazine ring to maintain the activity of nucleozin analogues. Interestingly, this coincides with a QSAR model developed here for the prediction of the anti-influenza activity. The proposed model, along with the synthetic route, will be useful for further development of nucleozin analogues with antiviral activity.