THE IMPORTANCE OF DRUG-MEMBRANE INTERACTION IN DRUG RESEARCH-AND-DEVELOPMENT

The importance of the interaction of drug molecules with membranes is discussed. The first two examples use the interaction of benzylpyrimidines with membranes of sensitive and resistant E. coli. This leads to a partial inactivation due to binding and to a change in mechanism of action, respectively. Another example deals with the interaction of amphiphilic benzylamines with artificial bilayers which lead to a change in conformation. The neuroleptic activity of Flupirtin derivatives could be described by the degree of interaction with bilayers quantified by NMR technique and a newly developed HPLC technique. Finally the interaction of amphiphilic drugs with membranes, possibly responsible for reversal of multidrug resistance in tumor and malaria therapy, is discussed.