New cis-Configured Aziridine-2-carboxylates as Aspartic Acid Protease Inhibitors (pages 141–152)
Dr. Christian Büchold, Yasmin Hemberger, Cornelia Heindl, Armin Welker, Dr. Björn Degel, Dr. Thomas Pfeuffer, Dr. Peter Staib, Sabrina Schneider, Prof. Dr. Philip J. Rosenthal, Dr. Jiri Gut, Prof. Dr. Joachim Morschhäuser, Prof. Dr. Gerhard Bringmann and Prof. Dr. Tanja Schirmeister
Article first published online: 16 NOV 2010 | DOI: 10.1002/cmdc.201000370
Sapping SAP activity:N-Alkyl-3-phenylaziridine-2-carboxylates are highly active inhibitors of cathepsin D and secreted aspartic acid protease 2 (SAP2). Syntheses, biological activity, and determination of the absolute configurations of the stereocenters by experimental circular dichroism (CD) and computational quantum chemical CD are presented herein.