Anne Cleasby

The Discovery of Novel Protein Kinase Inhibitors by Using Fragment-Based High-Throughput X-ray Crystallography

This article describes the application of a high‐throughput X‐ray crystallographic fragment‐based screening methodology to identify low‐molecular‐weight leads for structure‐based optimisation into protein kinase inhibitors. The identification of two novel p38α MAP kinase inhibitors (with IC50=65 and 150 nM) starting from low‐molecular‐weight fragments is described.

4-Acetylamino-3-(imidazol-1-yl)-benzoic acids as novel inhibitors of influenza sialidase

Two methods for the synthesis of 4-acetylamino benzoic acids substituted at the 3-position with imidazoles are described. Many of the compounds are inhibitors of influenza virus sialidases with levels of activity similar to the recently described 4-acetylamino-3-guanidino-benzoic acid (BANA 113).