Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374300 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Three different types of homobivalent compounds, 5,8,9,13b-tetrahydro-6H-isoqino[1,2-a]isoquinolines bearing tertiary N-atoms, their quaternary ammonium salts and their dibenzazecine analogues, connected by alkylene spacers of various lengths were synthesized. Compared to the therapeutically used inhibitor galanthamine, some of the bivalent compounds showed much higher inhibitory activities at both cholinesterases in the Ellman test. Surprisingly, not only the quaternary salts, but also the uncharged tertiary compounds exhibited IC50 values at butyrylcholinesterase in the nanomolar range. Selectivity toward BChE of up to 76-fold was observed.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Maria Schulze, Oliver Siol, Michael Decker, Jochen Lehmann,