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

Research output: Contribution to journalArticle

26 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.
LanguageEnglish
Pages1802-1815
Number of pages14
JournalBioorganic and Medicinal Chemistry
Volume19
Issue number5
DOIs
Publication statusPublished - 1 Mar 2011

Fingerprint

African Trypanosomiasis
Trypanosoma brucei brucei
Benzodiazepines
Libraries
Parasites
Bz-423

Keywords

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

Cite this

Spencer, John ; Rathnam, Rajendra P. ; Harvey, Alan L. ; Clements, Carol J. ; Clark, Rachel L. ; Barrett, Michael P. ; Wong, Pui Ee ; Male, Louise ; Coles, Simon J. ; Mackay, Simon P. / Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity. In: Bioorganic and Medicinal Chemistry . 2011 ; Vol. 19, No. 5. pp. 1802-1815.
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Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity. / Spencer, John; Rathnam, Rajendra P.; Harvey, Alan L.; Clements, Carol J.; Clark, Rachel L.; Barrett, Michael P.; Wong, Pui Ee; Male, Louise; Coles, Simon J.; Mackay, Simon P.

In: Bioorganic and Medicinal Chemistry , Vol. 19, No. 5, 01.03.2011, p. 1802-1815.

Research output: Contribution to journalArticle

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