title: Facile Synthesis and Preliminary Structure-Activity Analysis of New Sulfonamides Against Trypanosoma brucei.
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.
authors.affiliation: School of Chemistry, University of Wollongong , Wollongong 2522, Australia.
authors.forename: Adel A
authors.initials: AA
authors.lastname: Rashad
authors.affiliation: Eskitis Institute for Drug Discovery, Griffith University , Brisbane Innovation Park, Don Young Road, Nathan 4111, Australia.
authors.forename: Amy J
authors.initials: AJ
authors.lastname: Jones
authors.affiliation: Eskitis Institute for Drug Discovery, Griffith University , Brisbane Innovation Park, Don Young Road, Nathan 4111, Australia.
authors.forename: Vicky M
authors.initials: VM
authors.lastname: Avery
authors.affiliation: Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University , 381 Royal Parade, Parkville 3052, Australia.
authors.forename: Jonathan
authors.initials: J
authors.lastname: Baell
authors.affiliation: School of Chemistry, University of Wollongong , Wollongong 2522, Australia.
authors.forename: Paul A
authors.initials: PA
authors.lastname: Keller
keywords: SAR; T. brucei; sulfonamides; tetrahydroquinoline