Synthesis, antifungal activity and QSAR study of 2-arylhydroxynitroindoles

Eur J Med Chem. 2011 Sep;46(9):4374-82. doi: 10.1016/j.ejmech.2011.07.008. Epub 2011 Jul 19.


A series of 2-arylhydroxynitroindoles were prepared and tested for antifungal activity in vitro. The preliminary bioassays indicated that some compounds are comparable to the commercial fungicide (triadimefon). To further explore the structure-activity relationships, the data set of the seventeen structures and their quantitative values of antifungal activities were used for QSAR modeling. Based on the obtained QSAR models four new chemical compounds were designed, synthesized and tested in fungicidal assays. Reasonable correspondence between the experimental and predicted values of antifungal activity was observed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Magnetic Resonance Spectroscopy
  • Microbial Sensitivity Tests
  • Quantitative Structure-Activity Relationship


  • Antifungal Agents
  • Indoles