Structural analysis of chloroquine resistance reversal by imipramine analogs

Antimicrob Agents Chemother. 2001 Sep;45(9):2655-7. doi: 10.1128/AAC.45.9.2655-2657.2001.

Abstract

For imipramine, desipramine, and eight analogs of these well-known drugs, an N-5-aminoalkyl substitution was a minimum but insufficient structural feature associated with chloroquine resistance reversal. Although a second distal aliphatic nitrogen atom was unnecessary for resistance reversal, the direction of the dipole moment vector was critical.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Antimalarials / pharmacology*
  • Chloroquine / pharmacology*
  • Desipramine / pharmacology
  • Drug Interactions
  • Drug Resistance
  • Humans
  • Imipramine / analogs & derivatives
  • Imipramine / pharmacology*
  • Models, Molecular
  • Parasitic Sensitivity Tests
  • Plasmodium falciparum / drug effects*

Substances

  • Antimalarials
  • Chloroquine
  • Imipramine
  • Desipramine