Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity

John Spencer, Rajendra P. Rathnam, Alan L. Harvey, Carol J. Clements, Rachel L. Clark, Michael P. Barrett, Pui Ee Wong, Louise Male, Simon J. Coles, Simon P. Mackay

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27 Citations (Scopus)

Abstract

A library of 1,4-benzodiazepines has been synthesized and evaluated against Trypanosoma brucei, a causative parasite of Human African trypanosomiasis. Benzodiazepines possessing a P2- transporter motif were found to have MIC values as low as 0.78 μM.
Original languageEnglish
Pages (from-to)1802-1815
Number of pages14
JournalBioorganic and Medicinal Chemistry
Volume19
Issue number5
DOIs
Publication statusPublished - 1 Mar 2011

Keywords

  • synthesis
  • biological evaluation
  • 1,4-benzodiazepin-2-ones
  • antitrypanosomal activity
  • parallel synthesis
  • trypanosoma
  • benzodiazepines
  • microwaves

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    Spencer, J., Rathnam, R. P., Harvey, A. L., Clements, C. J., Clark, R. L., Barrett, M. P., Wong, P. E., Male, L., Coles, S. J., & Mackay, S. P. (2011). Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity. Bioorganic and Medicinal Chemistry , 19(5), 1802-1815. https://doi.org/10.1016/j.bmc.2011.01.010