Abstract
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 ?M range were revealed with a selectivity index suitable for further development.
Original language | English |
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Pages (from-to) | 496 - 500 |
Number of pages | 5 |
Journal | ACS Medicinal Chemistry Letters |
Volume | 5 |
Issue number | 5 |
DOIs | |
Publication status | Published - 2014 |