Identification of an Acridine Photoaffinity Probe for Trypanocidal Action

Academic Article

Abstract

  • Twenty-four acridine derivatives were screened for trypanocidal activity in Trypanosoma brucei in order to determine which structural features of the acridine molecule confer maximal antiparasitic activity. The syntheses of several new azidoacridine derivatives are also reported as well as an assessment of their value as possible photoaffinity probes for the study of acridine trypanocidal action. The most effective and selective acridine trypanocides, with and without irradiation, were the 3-amino-10-methylacridinium salt derivatives. With brief irradiation, one azidoacridine, 3-amino-6-azido-10-methylacridinium chloride, showed considerable trypanocidal activity at very limiting drug concentrations (10-7 M) and warrants consideration as a possible photoaffinity probe. © 1984, American Chemical Society. All rights reserved.
  • Published In

    Digital Object Identifier (doi)

    Pubmed Id

  • 14682897
  • Author List

  • Firth WJ; Messa A; Reid R; Charles Wang RC; Watkins CL; Yielding LW
  • Start Page

  • 865
  • End Page

  • 870
  • Volume

  • 27
  • Issue

  • 7