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

Journal Article


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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 μM range were revealed with a selectivity index suitable for further development.

Authors


  •   Rashad, Adel (external author)
  •   Jones, Amy J. (external author)
  •   Avery, Vicky M. (external author)
  •   Baell, Jonathan (external author)
  •   Keller, Paul A.

Publication Date


  • 2014

Citation


  • 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.

Scopus Eid


  • 2-s2.0-84900414255

Ro Full-text Url


  • http://ro.uow.edu.au/cgi/viewcontent.cgi?article=2798&context=smhpapers

Ro Metadata Url


  • http://ro.uow.edu.au/smhpapers/1780

Number Of Pages


  • 4

Start Page


  • 496

End Page


  • 500

Volume


  • 5

Issue


  • 5

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


  •   Rashad, Adel (external author)
  •   Jones, Amy J. (external author)
  •   Avery, Vicky M. (external author)
  •   Baell, Jonathan (external author)
  •   Keller, Paul A.

Publication Date


  • 2014

Citation


  • 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.

Scopus Eid


  • 2-s2.0-84900414255

Ro Full-text Url


  • http://ro.uow.edu.au/cgi/viewcontent.cgi?article=2798&context=smhpapers

Ro Metadata Url


  • http://ro.uow.edu.au/smhpapers/1780

Number Of Pages


  • 4

Start Page


  • 496

End Page


  • 500

Volume


  • 5

Issue


  • 5