Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1273-6. doi: 10.1016/s0960-894x(03)00109-4.

Abstract

The development of a series of novel indole-based inhibitors of 5'-inosine monophosphate dehydrogenase (IMPDH) is described. Various hydrogen bond acceptors at C-3 of the indole were explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are outlined.

MeSH terms

  • Cell Division / drug effects
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Glucuronides / metabolism
  • Humans
  • Hydrogen Bonding
  • IMP Dehydrogenase / antagonists & inhibitors*
  • Immune System / drug effects
  • Indoles / chemistry*
  • Isoenzymes / antagonists & inhibitors
  • Mitogens / pharmacology
  • Quinolones / chemical synthesis
  • Quinolones / pharmacology
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Glucuronides
  • Indoles
  • Isoenzymes
  • Mitogens
  • Quinolones
  • IMP Dehydrogenase