Activity of cationically substituted bis-benzimidazoles against experimental Pneumocystis carinii pneumonia

Antimicrob Agents Chemother. 1993 Aug;37(8):1713-6. doi: 10.1128/AAC.37.8.1713.

Abstract

On the basis of a previously observed correlation between the antimicrobial activity and DNA binding strength of dicationic molecules, a series of 10 dicationically substituted bis-benzimidazoles were tested for activity in the rat model of Pneumocystis carinii pneumonia. One of the compounds, 1,4-bis[5-(2-imidazolinyl)-2-benzimidazolyl]butane, was found to be more potent and less toxic than pentamidine.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Benzimidazoles / adverse effects
  • Benzimidazoles / metabolism
  • Benzimidazoles / pharmacology*
  • Cations / pharmacology
  • DNA / metabolism
  • Disease Models, Animal
  • Lung / anatomy & histology
  • Lung / drug effects
  • Male
  • Organ Size / drug effects
  • Pneumonia, Pneumocystis / drug therapy*
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship

Substances

  • Benzimidazoles
  • Cations
  • DNA