Bioorganic and Medicinal Chemistry Letters p. 377 - 379 (2012)
Update date:2022-08-03
Topics:
Dou, Dengfeng
He, Guijia
Mandadapu, Sivakoteswara Rao
Aravapalli, Sridhar
Kim, Yunjeong
Chang, Kyeong-Ok
Groutas, William C.
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.
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