Inhibition of noroviruses by piperazine derivatives.

ABSTRACT: There is currently an unmet need for the development of small-molecule therapeutics for norovirus infection. The piperazine scaffold, a privileged structure embodied in many 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 demonstrate for the first time that functionalized piperazine derivatives possess anti-norovirus activity. Furthermore, these studies have led to 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.

SUBMITTER: Dou D 

PROVIDER: S-EPMC3248970 | biostudies-literature | 2012 Jan

REPOSITORIES: biostudies-literature