Antiplasmodial Activity of Mono- and Dimeric Carbazoles

Gerhard Bringmann; Alfons Ledermann; Jörg Holenz; Muh-Tsuen Kao; Ulrich Busse; Howard G. Wu; Guido François

doi:10.1055/s-2006-957366

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Planta Med 1998; 64(1): 54-57
DOI: 10.1055/s-2006-957366

Papers

Natural Product Chemistry
© Georg Thieme Verlag Stuttgart · New York

Antiplasmodial Activity of Mono- and Dimeric Carbazoles

Gerhard Bringmann¹ , Alfons Ledermann¹ , Jörg Holenz¹ , Muh-Tsuen Kao² , Ulrich Busse³ , Howard G. Wu⁴ , Guido François⁵

¹Institut für Organische Chemie der Universität, Würzburg, Germany
²173, Jin-Wen Street, Wen-Shan District, Taipei, Taiwan, R.O.C.
³BASF AC, APE/EF - Li 444, Limburgerhof, Germany
⁴BASF Taiwan Ltd., Taipei, Taiwan, R.O.C.
⁵Prins Leopold Instituut voor Tropische Geneeskunde, Antwerpen, Belgium

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Publication History

1997

1997

Publication Date:
04 January 2007 (online)

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Abstract

A series of mono-and dimeric natural and structurally modified carbazoles has been tested for activity against Plasmodium falciparum. One of the monomers, the synthetic compound 1,4-diacetoxy-3-methylcarbazole (17), displays the highest activity, with an IC₅₀ value of 1.79 µg/ml. It is distinctly more active than the as yet best natural compound, 1-hydroxy-3-methylcarbazole (4) (4).

Key words

Murraya euchrestifolia - Rutaceae - Carbazoles - Murraya alkaloids - murrayafoline A - bismurrayaquinone A - koenoline - antiplasmodial activity - Plasmodium falciparum - human malaria