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

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
JournalA C S Medicinal Chemistry Letters
Volume5
Issue number5
DOIs
Publication statusPublished - 2014

Cite this

Rashad, Adel A ; Jones, Amy J ; Avery, Vicky M ; Baell, Jonathan Bayldon ; Keller, Paul Anthony. / Facile synthesis and preliminary structure-activity analysis of new sulfonamides against Trypanosoma brucei. In: A C S Medicinal Chemistry Letters. 2014 ; Vol. 5, No. 5. pp. 496 - 500.
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Facile synthesis and preliminary structure-activity analysis of new sulfonamides against Trypanosoma brucei. / Rashad, Adel A; Jones, Amy J; Avery, Vicky M; Baell, Jonathan Bayldon; Keller, Paul Anthony.

In: A C S Medicinal Chemistry Letters, Vol. 5, No. 5, 2014, p. 496 - 500.

Research output: Contribution to journalArticleResearchpeer-review

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AU - Keller, Paul Anthony

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