Inhibition of noroviruses by piperazine derivatives
Mandadapu, Sivakoteswara Rao
Groutas, William C.
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Dou, D., G. He, S.R. Mandadapu, S. Aravapalli, Y. Kim, K.O. Chang, and W.C. Groutas. 2012. "Inhibition of noroviruses by piperazine derivatives". Bioorganic & Medicinal Chemistry Letters. 22 (1): 377-379.
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 9I) that can be used as a launching pad for the optimization of potency, cytotoxicity, and drug-like characteristics.
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