Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT

Rachel L. Clark, Carol J. Clements, Michael P. Barrett, Simon P. Mackay, Rajendra P. Rathnam, George Owusu-Dapaah, John Spencer, Judith K. Huggan

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

A library of 1,4-benzodiazepines has been synthesised and evaluated for activity against Trypanosoma brucei, a causative parasite of Human African Trypanosomiasis (HAT). The most potent of these derivatives has an MIC value of 0.97 mu M. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds. (C) 2012 Elsevier Ltd. All rights reserved.

Original languageEnglish
Pages (from-to)6019-6033
Number of pages15
JournalBioorganic and Medicinal Chemistry
Volume20
Issue number20
DOIs
Publication statusPublished - 15 Oct 2012

Keywords

  • identification
  • development
  • 1,4-benzodiazepin-2-one
  • quinazoline-2,4-dione scaffolds
  • submicromolar inhibitors
  • HAT
  • trypanosomiasis
  • benzodiazepines

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