Inside Cover: Seamless Integration of Dose‐Response Screening and Flow Chemistry: Efficient Generation of Structure–Activity Relationship Data of β‐Secretase (BACE1) Inhibitors (Angew. Chem. Int. Ed. 6/2014)
Michael Werner, Christoph Kuratli, Rainer E. Martin, Remo Hochstrasser, David Wechsler, Thilo Enderle, Alexander I. Alanine, Horst Vogel · Angewandte Chemie International Edition · 2014
Structure–activity relationship (SAR) data is a key requirement in modern medicinal chemistry for optimization of lead molecules to drug candidates. In their Communication on page 1704 ff., M. Werner, R. E. Martin, and co-workers demonstrate with beta-secretase that cycle times for SAR generation can be reduced from days to 60 minutes. This accelerated process was achieved by integrating compound synthesis, purification, quantification, and biological assaying into a fully automated flow-based system.