Some non-conventional biomolecular targets for diamidines. A short survey

Bioorg Med Chem. 2014 Apr 1;22(7):1983-92. doi: 10.1016/j.bmc.2014.02.049. Epub 2014 Mar 5.


Increasing the affinity of diamidines for AT-rich regions of DNA has long been an important goal of medicinal chemists who wanted to improve the antiparasitic and antifungal properties of that class of derivatives. In recent years it was demonstrated that diamidines could interfere with many other biomolecular targets including ion channels as well as enzymes and modulate some RNA-protein, DNA-protein, and protein-protein interactions. It is therefore not surprising that diamidines now emerge as novel potential drug candidates for the treatment of various diseases, i.a. neurodegenerative disorders, acidosis-related pathological conditions, hypertension, thrombosis, type 2 diabetes, myotonic dystrophy, and cancers. A summary of the most striking results obtained to date in those domains is presented is this review.

Keywords: Amidines; Enzymes; Ions channels; Nucleic acid–protein interactions; Protein–protein interactions.

Publication types

  • Review

MeSH terms

  • Amidines / chemistry
  • Amidines / pharmacology*
  • Amidines / therapeutic use*
  • Animals
  • DNA / antagonists & inhibitors
  • Diabetes Mellitus, Type 2 / drug therapy
  • Enzymes / metabolism
  • Humans
  • Hypertension / drug therapy
  • Ion Channels / antagonists & inhibitors
  • Myotonic Dystrophy / drug therapy
  • Neoplasms / drug therapy
  • Neurodegenerative Diseases / drug therapy
  • Proteins / antagonists & inhibitors
  • RNA / antagonists & inhibitors
  • Thrombosis / drug therapy


  • Amidines
  • Enzymes
  • Ion Channels
  • Proteins
  • RNA
  • DNA