Symmetrical and unsymmetrical analogues of isoxyl; active agents against Mycobacterium tuberculosis

Academic Article

Abstract

  • Symmetrical and unsymmetrical analogues of the antimycobacterial agent isoxyl-have been synthesized and tested against Mycobacterium tuberculosis H37Rv and Mycobacterium bovis BCG, some showing an increased bactericidal effect. In particular, compounds 1-(p-n-butylphenyl)-3-(4-propoxy-phenyl) thiourea (10) and 1-(p-n-butylphenyl)-3-(4-n-butoxy-phenyl) thiourea (11) showed an approximate 10-fold increase in in vitro potency compared to isoxyl, paralleled by increased inhibition of mycolic acid biosynthesis in M. bovis BCG. Interestingly, these isoxyl analogues showed relatively poor inhibition of oleate production, suggesting that the modifications have changed the spectrum of biological activity. © 2006 Elsevier Ltd. All rights reserved.
  • Digital Object Identifier (doi)

    Author List

  • Bhowruth V; Brown AK; Reynolds RC; Coxon GD; Mackay SP; Minnikin DE; Besra GS
  • Start Page

  • 4743
  • End Page

  • 4747
  • Volume

  • 16
  • Issue

  • 18