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

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 disulf...

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Published inACS medicinal chemistry letters Vol. 5; no. 5; pp. 496 - 500
Main Authors Rashad, Adel A, Jones, Amy J, Avery, Vicky M, Baell, Jonathan, Keller, Paul A
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 08.05.2014
Amer Chemical Soc
Subjects
Chemistry, Medicinal
Letter
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Science & Technology
T. brucei
sulfonamides
tetrahydroquinoline
SAR
HUMAN AFRICAN TRYPANOSOMIASIS
COMBINATION THERAPY
DRUG DISCOVERY
SLEEPING SICKNESS
ASPARTATE NMDA RECEPTOR
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Summary: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.
Bibliography:ObjectType-Article-1
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ISSN:1948-5875
1948-5875
DOI:10.1021/ml400487t