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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

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Inhibition of noroviruses by piperazine derivatives.

Dou Dengfeng D He Guijia G Mandadapu Sivakoteswara Rao SR Aravapalli Sridhar S Kim Yunjeong Y Chang Kyeong-Ok KO Groutas William C WC

Bioorganic & medicinal chemistry letters 20111115 1

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 ...[more]

PMID: 22119464

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