Tertiary‐Amine‐Based Inhibitors of the Astacin Protease Meprin α

• DOI: 10.1002/cmdc.201800300
• Publication Date: 2018-06-21T11:09:20Z
• Authors: Kathrin Tan; Christian Jäger; Dagmar Schlenzig; Stephan Schilling; Mirko Buchholz; Daniel Ramsbeck
• Keywords: Tertiary amine

Abstract Metalloproteinases of the astacin family are drawing ever increasing attention as potential drug targets. However, knowledge regarding inhibitors thereof is limited in most cases. Crucial for development metalloprotease high selectivity, to avoid side effects brought about by inhibition off‐target proteases and interference with physiological pathways. In this study we aimed at design novel selective proteinase meprin α. Based on a recently identified tertiary amine scaffold, series compounds was synthesized evaluated. The exhibit reasonable inhibitory activity selectivity over other metalloproteases. isoenzyme β only slightly inhibited. Hence, present revealed class α improved known compounds.