Facile synthesis and preliminary structure-activity analysis of new sulfonamides against Trypanosoma brucei

Adel A Rashad, Amy J Jones, Vicky M Avery, Jonathan Bayldon Baell, Paul Anthony Keller

Research output: Contribution to journalArticleResearchpeer-review

14 Citations (Scopus)

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 languageEnglish
Pages (from-to)496 - 500
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume5
Issue number5
DOIs
Publication statusPublished - 2014

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