Biological active acridine derivatives. Part 4: Synthesis and antiviral activity of some bis-acridinylated diamides

Pharmazie. 2000 Oct;55(10):733-6.

Abstract

Nine bis-acridine derivatives have been synthesized in search of structures with antiviral properties. Synthesis of target compounds was provided by a standard peptide-like coupling procedure using aliphatic diamines and protected amino acids following protective group removing and acridinylation by means of 9-methoxyacridine. Two out of nine compounds tested demonstrate high protective activity of Vero cells against HSV infection. Antiviral activity was observed only for compounds containing a pentamethylene fragment as a linker. The alanyl-containing derivative was less active than those containing valyl- and phenylalanyl. Most of synthesized compounds were less toxic than N,N'-bis-(acridinyl) hexamethylenediamine.

MeSH terms

  • Acridines / chemical synthesis*
  • Acridines / pharmacology
  • Animals
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Chlorocebus aethiops
  • Intercalating Agents / pharmacology
  • Microbial Sensitivity Tests
  • Simplexvirus / drug effects
  • Vero Cells

Substances

  • Acridines
  • Antiviral Agents
  • Intercalating Agents