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
Year published
2014
Metadata
Show full item recordAbstract
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
Subject
Medical and Health Sciences not elsewhere classified
Medicinal and Biomolecular Chemistry
Organic Chemistry
Pharmacology and Pharmaceutical Sciences