Bowden K, Harris N V, Watson C A
Department of Chemistry & Biological Chemistry, University of Essex, Colchester, U.K.
J Chemother. 1993 Dec;5(6):377-88.
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.
综述了抗菌二氢叶酸还原酶抑制剂的构效关系。首先进行了简短介绍，随后更详细地回顾了自1980年以来的进展。讨论了基于X射线晶体学、核磁共振光谱和分子图形学研究数据的定点抑制剂设计。从历史角度审视了定量构效关系的发展，并将其与最近的替代方法进行了对比。得出了关于未来可能发展的结论。
