ABSTRACT
The novel isosteric ribavirin analogues were synthesized by two different ways. Some of them showed significant antiviral action against hepatitis C virus (HCV), herpes simplex (HCV-1) and influenza A virus comparable to that of ribavirin itself. The data obtained confirm the proposed theory of the ribavirin possible antiviral activity mechanism related with bioisosterism.
Subject(s)
Antiviral Agents/chemical synthesis , Ribavirin/analogs & derivatives , Animals , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Cell Survival/drug effects , Chlorocebus aethiops , Hepacivirus/drug effects , Herpesvirus 1, Human/drug effects , Humans , Influenza A virus/drug effects , Ribavirin/chemical synthesis , Ribavirin/pharmacology , Vero CellsABSTRACT
Distribution coefficient (D) of rifabutin in liposome/water system was measured by phase separation and fluorescence probe quenching techniques. D values were identical suggesting that rifabutin is fully immersed into lipid bilayer. Structural studies of phospholipid bilayer employing (31)P NMR spectroscopy demonstrated that introduction of rifabutin does not alter the bilayer structure. A scheme of the rifabutin position in lipid bilayer based on the calculated size of rifabutin molecule is proposed.
