Structural analysis of chloroquine resistance reversal by imipramine analogs

A K Bhattacharjee; D E Kyle; J L Vennerstrom

doi:10.1128/AAC.45.9.2655-2657.2001

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.

Authors

A K Bhattacharjee¹, D E Kyle, J L Vennerstrom

Affiliation

¹ Department of Medicinal Chemistry, Walter Reed Army Institute of Research, Washington, DC 20307-5100, USA.

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