898413-88-2Relevant academic research and scientific papers
Facile Synthesis and Preliminary Structure-Activity Analysis of New Sulfonamides Against Trypanosoma brucei
Rashad, Adel A.,Jones, Amy J.,Avery, Vicky M.,Baell, Jonathan,Keller, Paul A.
, p. 496 - 500 (2014/06/09)
The high throughput screening of a library of over 87,000 drug-like compounds against the African sleeping sickness parasite resulted in the discovery of hits with a wide range of molecular diversity. We report here the medicinal chemistry development of one such hit, a tetrahydroisoquinoline disulfonamide, with the synthesis and testing of 26 derivatives against the trypanosome subspecies. Activities in the 2-4 μM range were revealed with a selectivity index suitable for further development.
