Antimalarial benzo[c]phenanthridines

Bioorg Med Chem Lett. 2005 Apr 15;15(8):2007-10. doi: 10.1016/j.bmcl.2005.02.074.

Abstract

Analogues of the antimalarial alkaloid nitidine have been prepared with high potency against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. Simple modifications, using an established synthetic route, resulted in an analogue with IC(50) below 5ng/mL against a chloroquine-sensitive strain of P. falciparum. N-Ethylethoxidine had IC(50) below 30ng/mL against both chloroquine-sensitive and chloroquine-resistant strains of P. falciparum.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Antimalarials / chemistry*
  • Antimalarials / pharmacology
  • Humans
  • Microbial Sensitivity Tests
  • Netropsin / chemistry
  • Netropsin / pharmacology
  • Phenanthridines / chemistry*
  • Phenanthridines / pharmacology
  • Plasmodium falciparum / drug effects*
  • Plasmodium falciparum / physiology

Substances

  • Antimalarials
  • Phenanthridines
  • ethoxidine
  • Netropsin