N1,N1-dimethyl-N3-(3-(trifluoromethyl) phenethyl)propane-1,3-diamine, a new lead for the treatment of human African trypanosomiasis

Article abstract of DOI:10.1016/j.ejmech.2013.12.050

The natural product, convolutamine I (1), has anti-trypanosomal activity however it has a high molecular weight of 473 due to a presence of 3 bromine atoms. The synthesis of the natural product convolutamine I (1) together with its analogues are presented. A SAR study against Trypanosoma brucei brucei led to compounds with improved physico-chemical properties: lower molecular weight and lower log P while maintaining potency (with a slight 2-fold improvement).