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A new class of compounds that exhibit anti-norovirus activity in a cell-based system and embody in their structure a cyclosulfamide scaffold has been identified. The structure of the initial hit (compound 2a, ED(50) 4 μM, TD(50) 50 μM) has been
Journal of the American Chemical Society, 134(26), 10807-10810 (2012-06-20)
Nitrogen-containing stereotriads, compounds with three adjacent stereodefined carbons, are commonly found in biologically important molecules. However, the preparation of molecules bearing these motifs can be challenging. Herein, we describe a modular oxidation protocol which converts a substituted allene to a
The last version of the PRECLAV algorithm was used to investigate a series of sulfamate/sulfamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. PRECLAV allows identification of outliers for lead hopping, significant molecular fragments and similarity computation of a calibration set vs.
A total synthesis of (-)-kaitocephalin, an ionotropic glutamate receptor antagonist, is accomplished in highly stereocontrolled manner via Overman rearrangement, rhodium-catalyzed benzylic C-H amination, pyrrolidine formation involving nucleophilic opening of a cyclic sulfamate, and rhodium-catalyzed allylic C-H amination as key steps.
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