Structure-activity relationships of dihydrofolate reductase inhibitors.
Structure-activity relationships of antibacterial dihydrofolate reductase inhibitors are reviewed. A short introduction is followed by a more detailed review of developments since 1980. The design of site directed inhibitors based on data from X-ray crystallographic, NMR spectroscopy and molecular graphic studies is discussed. The development of quantitative structure-activity relations is surveyed from a historical point of view and these are contrasted with more recent alternative approaches. Conclusions are reached regarding possible future developments.
Bowden
K
K
Department of Chemistry & Biological Chemistry, University of Essex, Colchester, U.K.
Harris
N V
NV
Watson
C A
CA
D000818:Animals; D000890:Anti-Infective Agents / Q000494:pharmacology*; D005493:Folic Acid Antagonists; D011621:Pteridines / Q000494:pharmacology; D011743:Pyrimidines / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000890:Anti-Infective Agents; D005493:Folic Acid Antagonists; D011621:Pteridines; D011743:Pyrimidines