Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2931-4. doi: 10.1016/s0960-894x(02)00600-5.

Abstract

A series of novel guanidine-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given.

MeSH terms

  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / pharmacology
  • Crystallography, X-Ray
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Guanidine / analogs & derivatives*
  • Guanidine / chemical synthesis*
  • Guanidine / pharmacology
  • Humans
  • IMP Dehydrogenase / antagonists & inhibitors*
  • Indicators and Reagents
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • Enzyme Inhibitors
  • Indicators and Reagents
  • IMP Dehydrogenase
  • Guanidine