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. 2025 May 8;86(3):e70095. doi: 10.1002/ddr.70095

SCHEME 4.

SCHEME 4

Structure‐activity relationships among aryl vinyl sulfones. Electron‐withdrawing groups on sulfur (R1) increase rate of inactivation. Aromatic and heteroaromatic rings (R2 in Scheme 2) are well tolerated at the β‐carbon, as is the alanyl group. Quinolines and pyridines with multiple regiochemical orientations of the nitrogen versus the vinyl group. H‐bond acceptors (R3) para with respect to the vinyl group improve binding.