Quinazolinone fungal efflux pump inhibitors. Part 2: In vitro structure-activity relationships of (N-methyl-piperazinyl)-containing derivatives

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5133-7. doi: 10.1016/j.bmcl.2004.07.071.

Abstract

Structure-activity relationships of a novel series of fungal efflux pump inhibitors with respect to potentiation of the activity of fluconazole against strains of Candida albicans and Candida glabrata over-expressing ABC-type efflux pumps are systematically explored.

Publication types

  • Comparative Study

MeSH terms

  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology
  • Candida / drug effects*
  • Candida / enzymology
  • Candida albicans / drug effects
  • Candida albicans / enzymology
  • Candida glabrata / drug effects
  • Candida glabrata / enzymology
  • Drug Resistance, Fungal
  • Drug Synergism
  • Fluconazole / chemistry
  • Fluconazole / pharmacology
  • Fungal Proteins / antagonists & inhibitors
  • Humans
  • Membrane Transport Modulators*
  • Membrane Transport Proteins / antagonists & inhibitors*
  • Microbial Sensitivity Tests
  • Piperazines / chemical synthesis*
  • Piperazines / chemistry
  • Piperazines / pharmacology
  • Quinazolines / chemical synthesis*
  • Quinazolines / chemistry
  • Quinazolines / pharmacology
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Antifungal Agents
  • CDR1 protein, Candida albicans
  • Fungal Proteins
  • Membrane Transport Modulators
  • Membrane Transport Proteins
  • Piperazines
  • Quinazolines
  • Fluconazole