0000000001316834
AUTHOR
William J. Robinson
The discovery of novel antitrypanosomal 4-phenyl-6-(pyridin-3-yl)pyrimidines
Human African trypanosomiasis, or sleeping sickness, is a neglected tropical disease caused by Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense which seriously affects human health in Africa. Current therapies present limitations in their application, parasite resistance, or require further clinical investigation for wider use. Our work herein describes the design and syntheses of novel antitrypanosomal 4-phenyl-6-(pyridin-3-yl)pyrimidines, with compound 13, the 4-(2-methoxyphenyl)-6-(pyridine-3-yl)pyrimidin-2-amine demonstrating an IC50 value of 0.38 μM and a promising off-target ADME-Tox profile in vitro. In silico molecular target investigations showed rhodesain to be a pu…
CCDC 2012793: Experimental Crystal Structure Determination
Related Article: William J. Robinson, Annie E. Taylor, Solange Lauga-Cami, George W. Weaver, Randolph R.J. Arroo, Marcel Kaiser, Sheraz Gul, Maria Kuzikov, Bernhard Ellinger, Kuldip Singh, Tanja Schirmeister, Adolfo Botana, Chatchakorn Eurtivong, Avninder S. Bhambra|2021|Eur.J.Med.Chem.|209|112871|doi:10.1016/j.ejmech.2020.112871