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Tertiary‐amine‐based inhibitors of the astacin protease meprin α

: Tan, Kathrin; Jäger, Christian; Schlenzig, Dagmar; Schilling, Stephan; Buchholz, Mirko; Ramsbeck, Daniel


ChemMedChem 13 (2018), No.16, pp.1619-1624
ISSN: 1860-7179
ISSN: 1860-7187
Journal Article
Fraunhofer IZI ()

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 the development of metalloprotease inhibitors is high selectivity, to avoid side effects brought about by inhibition of off‐target proteases and interference with physiological pathways. In this study we aimed at the design of novel selective inhibitors for the astacin proteinase meprin α. Based on a recently identified tertiary amine scaffold, a series of compounds was synthesized and evaluated. The compounds exhibit reasonable inhibitory activity with high selectivity over other metalloproteases. The isoenzyme meprin β is only slightly inhibited. Hence, the present study revealed a novel class of selective meprin α inhibitors with improved selectivity over known compounds.