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  • Facile Synthesis and Preliminary Structure–Activity Analysis of New Sulfonamides Against Trypanosoma brucei

    Author(s)
    Rashad, Adel A
    Jones, Amy J
    Avery, Vicky M
    Baell, Jonathan
    Keller, Paul A
    Griffith University Author(s)
    Avery, Vicky M.
    Jones, Amy J.
    Year published
    2014
    Metadata
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    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 μM range were revealed with a selectivity index suitable for further development.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.
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    Journal Title
    ACS Medicinal Chemistry Letters
    Volume
    5
    Issue
    5
    DOI
    https://doi.org/10.1021/ml400487t
    Subject
    Medical and Health Sciences not elsewhere classified
    Medicinal and Biomolecular Chemistry
    Organic Chemistry
    Pharmacology and Pharmaceutical Sciences
    Publication URI
    http://hdl.handle.net/10072/141071
    Collection
    • Journal articles

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