Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375593 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
Novel 2,3-diarylindoles bearing an amine substituent at the indole 5- and 6-positions have been synthesized and evaluated as anticoccidial agents in both in vitro and in vivo assays. Both subnanomolar in vitro activity and broad spectrum in vivo potency were detected for several compounds, particularly compound 27.
Graphical abstractIn this study, we present the synthesis and biological activity of 2,3-diarylindoles, whose antiparasitic activity against Eimeria is due to inhibition of a parasite specific cGMP-dependent protein kinase (PKG). From this series, several compounds showed subnanomolar in vitro activity and significant in vivo activity.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Andrew Scribner, Joseph A. Moore III, Gilles Ouvry, Michael Fisher, Matthew Wyvratt, Penny Leavitt, Paul Liberator, Anne Gurnett, Chris Brown, John Mathew, Donald Thompson, Dennis Schmatz, Tesfaye Biftu,