Synthesis and biological activity of anticoccidial agents: 2,3-diarylindoles

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.

In 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 as PowerPoint slide