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

doi:10.1021/ml400487t

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

Medicinal Chemistry

Research output: Contribution to journal › Article › Research › peer-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 language	English
Pages (from-to)	496 - 500
Number of pages	5
Journal	ACS Medicinal Chemistry Letters
Volume	5
Issue number	5
DOIs	https://doi.org/10.1021/ml400487t
Publication status	Published - 2014

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10.1021/ml400487t

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Cite this

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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 ?M range were revealed with a selectivity index suitable for further development.",

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AU - Baell, Jonathan Bayldon

AU - Keller, Paul Anthony

PY - 2014

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AB - 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.

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JO - ACS Medicinal Chemistry Letters

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