Facile synthesis and preliminary structure-activity analysis of new sulfonamides against Trypanosoma brucei

Authors

Adel Rashad, University of WollongongFollow
Amy J. Jones, Griffith University
Vicky M. Avery, Griffith University
Jonathan Baell, Monash University
Paul Keller, University of WollongongFollow

RIS ID

90331

Publication Details

Rashad, A. A., Jones, A. J., Avery, V. M., Baell, J. & Keller, P. A. (2014). Facile synthesis and preliminary structure-activity analysis of new sulfonamides against Trypanosoma brucei. ACS Medicinal Chemistry Letters, 5 (5), 496-500.

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.