From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds

Muthusamy Venkatraj, Kevin Ariën, Jan Heeres, Jurgen Joossens, Bertrand Dirié, Sophie Lyssens, Johan Michiels, Paul Cos, Paul J Lewi, Guido Vanham, Louis Maes, Pieter Van der Veken, Koen Augustyns

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Abstract

The presence of a structural recognition motif for the nucleoside P2 transporter in a library of pyrimidine and triazine non-nucleoside HIV-1 reverse transcriptase inhibitors, prompted for the evaluation of antitrypanosomal activity. It was demonstrated that the structure-activity relationship for anti-HIV and antitrypanosomal activity was different. Optimization in the diaryl triazine series led to 6-(mesityloxy)-N2-phenyl-1,3,5-triazine-2,4-diamine (69), a compound with potent in vitro and moderate in vivo antitrypanosomal activity.

Original languageEnglish
JournalBioorganic and Medicinal Chemistry
Volume22
Issue number19
Pages (from-to)5241-5248
Number of pages8
ISSN0968-0896
DOIs
Publication statusPublished - 2014

Keywords

  • Anti-HIV Agents
  • Cell Line
  • Cell Survival
  • Dose-Response Relationship, Drug
  • HIV Reverse Transcriptase
  • HIV-1
  • Humans
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Parasitic Sensitivity Tests
  • Reverse Transcriptase Inhibitors
  • Structure-Activity Relationship
  • Trypanocidal Agents
  • Trypanosoma brucei brucei
  • Trypanosoma brucei rhodesiense

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