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Evaluation of cryptolepine and huperzine derivatives as lead compounds towards new agents for the treatment of human African Trypanosomiasis.

By A.J. Oluwafemi, O. Okanla, P. Camps, D. Muñoz-Torrero, Z.B. Mackey, P.K. Chiang, Scott Seville and Colin W. Wright


noThe alkaloid cryptolepine (1) and eight synthetic analogues (2-8) were assessed for in vitro activities against Trypanosoma brucei. Four of the analogues were found to be highly potent with IC50 values of less than 3 nM and three of these were assessed against T. brucei brucei infection in rats. The most effective compound was 2,7-dibromocryptolepine (7); a single oral dose of 20 mg/Kg suppressed parasitaemia and increased the mean survival time to 13.6 days compared with 8.4 days for untreated controls. In addition, four huperzine derivatives (9-12) were shown to have in vitro antitrypanosomal activities with IC50 values from 303-377 nM

Topics: Sleeping sickness, Trypanosoma brucei, Cryptolepine derivatives, Huperzine derivatives, Trypanosomiasis
Publisher: Natural Products Inc.
Year: 2009
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Provided by: Bradford Scholars
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