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Antimicrobial Agents and Chemotherapy, September 2001, p. 2655-2657, Vol. 45, No. 9
0066-4804/01/$04.00+0   DOI: 10.1128/AAC.45.9.2655-2657.2001
Copyright © 2001, American Society for Microbiology. All rights reserved.

Structural Analysis of Chloroquine Resistance Reversal by Imipramine Analogs

Apurba K. Bhattacharjee,1 Dennis E. Kyle,2 and Jonathan L. Vennerstrom3,*

Department of Medicinal Chemistry1 and Department of Parasitology,2 Walter Reed Army Institute of Research, Washington, D.C. 20307-5100, and College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska 68198-60253

Received 4 April 2001/Returned for modification 21 May 2001/Accepted 18 June 2001

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.

* Corresponding author. Mailing address: College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE 68198-6025. Phone: (402) 559-5362. Fax: (402) 559-9543. E-mail: jvenners{at}unmc.edu.

Antimicrobial Agents and Chemotherapy, September 2001, p. 2655-2657, Vol. 45, No. 9
0066-4804/01/$04.00+0   DOI: 10.1128/AAC.45.9.2655-2657.2001
Copyright © 2001, American Society for Microbiology. All rights reserved.


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