1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation

Eur J Med Chem. 2014 Nov 24:87:801-4. doi: 10.1016/j.ejmech.2014.10.024. Epub 2014 Oct 13.

Abstract

1H-1,2,3-triazole tethered isatin-ferrocene conjugates were synthesized and evaluated for their antiplasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The conjugates 5f and 5h with an optimum combination of electron-withdrawing halogen substituent at C-5 position of isatin ring and a propyl chain, introduced as linker, proved to be most potent and non-cytotoxic among the series with IC50 values of 3.76 and 4.58 μM against 3D7 and W2 strains, respectively.

Keywords: Antimalarial evaluation; Click chemistry; Cytotoxicity; Isatin-ferrocene conjugates; Structure activity relationship.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Ferrous Compounds / chemistry*
  • Isatin / chemistry*
  • Metallocenes
  • Structure-Activity Relationship
  • Triazoles / chemistry*

Substances

  • Antimalarials
  • Ferrous Compounds
  • Metallocenes
  • Triazoles
  • Isatin
  • ferrocene