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Antimicrobial Agents and Chemotherapy, March 2002, p. 882-883, Vol. 46, No. 3
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.3.882-883.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

Antitrypanosomal Activities of Tryptanthrins

John Scovill,1 Elizabeth Blank,1 Michael Konnick,1 Elizabeth Nenortas,2 and Theresa Shapiro2*

Department of Chemistry, Bucknell University, Lewisburg, Pennsylvania 17837,1 Division of Clinical Pharmacology, Department of Medicine, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205-21852

Received 18 April 2001/ Returned for modification 18 June 2001/ Accepted 28 November 2001

New drugs and molecular targets are needed against Trypanosoma brucei, the protozoan that causes African sleeping sickness. Tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione), a traditional antifungal agent, and 11 analogs were tested against T. brucei in vitro. The greatest activity was conferred by electron-withdrawing groups in the 8 position of the tryptanthrin ring system; the most potent compound had a 50% effective concentration of 0.40 µM.

* Corresponding author. Mailing address: Johns Hopkins School of Medicine, 303 Hunterian Building, 725 North Wolfe St., Baltimore, MD 21205. Phone: (410) 955-1888. Fax: (410) 955-2634. E-mail: tshapiro{at}jhmi.edu.

Antimicrobial Agents and Chemotherapy, March 2002, p. 882-883, Vol. 46, No. 3
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.3.882-883.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.



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