A new class of type I protein geranylgeranyltransferase (GGTase I) inhibitor

Bioorg Med Chem Lett. 2002 Feb 25;12(4):629-32. doi: 10.1016/s0960-894x(01)00813-7.

Abstract

Replacement of the thiol groups in 1, a potent and highly selective Candida albicans GGTase I inhibitor discovered through screening, with an imidazole ring was achieved by using solid phase synthesis. A non-thiol compound, 7, was found as a representative of a new class of potent C. albicans GGTase I inhibitor with high selectivity against human GGTase I.

MeSH terms

  • Antifungal Agents / chemistry
  • Antifungal Agents / classification
  • Antifungal Agents / pharmacology
  • Candida albicans / enzymology
  • Combinatorial Chemistry Techniques*
  • Dipeptides
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / classification
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Imidazoles
  • Inhibitory Concentration 50
  • Structure-Activity Relationship

Substances

  • Antifungal Agents
  • Dipeptides
  • Enzyme Inhibitors
  • Imidazoles
  • imidazole