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

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.