Inhibition of noroviruses by piperazine derivatives.

The piperazine scaffold, a privileged structure embodied in a range of pharmacological agents, was used to synthesize an array of structurally-diverse derivatives which were screened for anti-norovius activity in a cell-based replicon system. The studies described herein have demonstrated that piperazine derivatives posses anti-norovirus activity. Furthermore, these studies have resulted in the identification of two promising compounds (6a and 9l) that can be used as a launching pad for the optimization of potency, cytotoxicity, and drug-like characteristics.