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Structure-activity relationships of dihydrofolate reductase inhibitors

Bowden, K.; Harris, N.V.; Watson, C.A.

Journal of ChemoTherapy 5(6): 377-388

1993

ISSN/ISBN: 1120-009X
PMID: 8195829
Document Number: 411778
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.

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