Christian Alan Paul Smethurst

Synthesis and structure of bifunctional N-alkylbenzimidazole phenylboronate derivatives

N-Methyl and N-n-butyl-2-(2-boronophenyl)benzimidazoles are accessed from the corresponding mono-N-alkyl-ortho-phenylenediamines, either using a polyphosphoric acid-mediated cyclisation with ortho-bromobenzoic acid, or preferably using an Oxone-mediated cyclisation of the corresponding aldehyde, followed by a lithium-exchange and borylation sequence. The resulting boronic acids show unusual physical and chemical properties, as shown by 11B NMR and X-ray crystallography.

Small molecule antagonism of oxysterol-induced Epstein-Barr virus induced gene 2 (EBI2) activation.

The Epstein–Barr virus induced gene 2 (EBI2) was recently identified as the first oxysterol‐activated 7TM receptor. EBI2 is essential for B cell trafficking within lymphoid tissues and thus the humoral immune response in general. Here we characterize the antagonism of the non‐peptide molecule GSK682753A, which blocks oxysterol‐induced G‐protein activation, β‐arrestin recruitment and B‐cell chemotaxis. We furthermore demonstrate that activation triggers pertussis toxin‐sensitive MAP kinase phosphorylation, which is also inhibited by GSK682753A. Thus, EBI2 signalling in B cells mediates key phenotypic functions via signalling pathways amenable to manipulation providing additional therapeutic options for inhibiting EBI2 activity.

Potassium 4-nitro­phenyl­sulfonate monohydrate

The title compound, K+·C6H4NO5S−·H2O, forms a three-dimensional polymeric structure with an O8 coordination environment of the K+ cation.