Cyclosulfamide-based derivatives as inhibitors of noroviruses
Mandadapu, Sivakoteswara Rao
Alliston, Kevin R.
Groutas, William C.
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European journal of medicinal chemistry. 2011 Oct 20. [Epub ahead of print]
An optimization campaign focused on improving pharmacological activity and physicochemical properties of a recently-identified class of cyclosulfamide-based norovirus inhibitors has been carried out. Dimeric compound 4 was found to be a ~10-fold more potent norovirus inhibitor (ED(50) 0.4 µM) compared to the original hit, however, isonipecotic acid ester derivatives 7e and 10a were shown to have superior therapeutic indices.
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