Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues

Bioorg Med Chem Lett. 2003 Feb 10;13(3):547-51. doi: 10.1016/s0960-894x(02)00945-9.


The synthesis and the structure-activity relationships (SAR) of analogues derived from the introduction of basic residues on ring D of quinolone-based inhibitors of IMPDH are described. This led to the identification of compound 27 as a potent inhibitor of IMPDH with significantly improved aqueous solubility over the lead compound 1.

MeSH terms

  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • IMP Dehydrogenase / antagonists & inhibitors*
  • Quinolones / chemical synthesis*
  • Quinolones / pharmacology*
  • Stereoisomerism
  • Structure-Activity Relationship


  • Enzyme Inhibitors
  • Quinolones
  • IMP Dehydrogenase