Article
Identification and validation of tetracyclic benzothiazepines as Plasmodium falciparum cytochrome bc1 inhibitors.
Chemistry & biology - 23 Dec 2011
Dong Carolyn K, Urgaonkar Sameer, Cortese Joseph F, Gamo Francisco-Javier, Garcia-Bustos Jose F, Lafuente Maria J, Patel Vishal, Ross Leila, Coleman Bradley I, Derbyshire Emily R, Clish Clary B, Serrano Adelfa E, Cromwell Mandy, Barker Robert H, Dvorin Jeffrey D, Duraisingh Manoj T, Wirth Dyann F, Clardy Jon, Mazitschek Ralph
Abstract excerpt
Here we report the discovery of tetracyclic benzothiazepines (BTZs) as highly potent and selective antimalarials along with the identification of the Plasmodium falciparum cytochrome bc(1) complex as the primary functional target of this novel compound class. Investigation of the structure activity relationship within this previously unexplored chemical scaffold has yielded inhibitors with low nanomolar activity....
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