STRUCTURE-ACTIVITY-RELATIONSHIPS OF DIHYDROFOLATE-REDUCTASE INHIBITORS

Structure activity relationships of antibacterial dihydrofolate reduct ase inhibitors are reviewed. A short introduction is followed by a mor e detailed review of developments since 1980. The design of site direc ted inhibitors based on data from X-ray crystallographic, NMR spectros copy and molecular graphic studies is discussed. The development of qu antitative structure-activity relations is surveyed from a historical point of view and these are contrasted with more recent alternative ap proaches. Conclusions are reached regarding possible future developmen ts.