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Phenazines with two cationic side chains as potential antimalarials.

S N Sawhney, D W Boykin

    Journal of Pharmaceutical Sciences
    |April 1, 1979
    PubMed
    Summary
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    New phenazine compounds were synthesized and tested for antimalarial activity. Unfortunately, these potential antimalarials showed no significant activity against Plasmodium berghei, indicating limited therapeutic value.

    Area of Science:

    • Medicinal Chemistry
    • Parasitology
    • Organic Synthesis

    Background:

    • Malaria remains a significant global health challenge, necessitating the development of novel therapeutic agents.
    • Phenazine derivatives have been explored for various biological activities, including potential antimalarial properties.

    Purpose of the Study:

    • To synthesize novel 1,9-Phenazine-bis(dialkylaminocarboxamides) as potential antimalarial drug candidates.
    • To evaluate the in vitro efficacy of these synthesized compounds against Plasmodium berghei.

    Main Methods:

    • Synthesis of phenazine targets from 1,9-phenazinedicarboxylic acid using standard organic chemistry techniques.
    • Screening of synthesized compounds for antimalarial activity against Plasmodium berghei.

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    Main Results:

    • The synthesized 1,9-Phenazine-bis(dialkylaminocarboxamides) did not exhibit significant antimalarial activity against Plasmodium berghei.
    • An unexpected side reaction occurred during synthesis, yielding 4-chloro-1,9-phenazinedicarbonyl chloride from 1,9-phenazinedicarboxylic acid and thionyl chloride.

    Conclusions:

    • The tested phenazine derivatives are not effective antimalarial agents against Plasmodium berghei.
    • Further structural modifications or alternative synthetic routes may be required to develop effective phenazine-based antimalarials.