Facile Synthesis and Preliminary Structure–Activity Analysis of New Sulfonamides Against Trypanosoma brucei
MetadataShow full item record
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.
ACS Medicinal Chemistry Letters
Medical and Health Sciences not elsewhere classified