Abstract
New pyranonaphthoquinone derivatives were synthesized and investigated for their activity against Trypanosoma brucei, Leishmania major, and Toxoplasma gondii parasites. The pentafluorophenyl derivative was efficacious against T. brucei with single digit micromolar EC50 values and against T. gondii with even sub-micromolar values. The 3-chloro-4,5-dimethoxyphenyl derivative showed an activity against amastigotes of Leishmania major parasites comparable to that of amphotericin B. In addition, antioxidant activities were observed for the bromophenyl derivatives, and their redox behavior was studied by cyclovoltammetry. Anti-parasitic and antioxidative activities of the new naphthoquinone derivatives appear uncorrelated.
Highlights
Infections of immune-compromised patients and newborn children with the world-wide occurring toxoplasmosis can lead to severe complications and, efficient drugs for the treatment of toxoplasmosis are necessary.[1]
Human African trypanosomiasis (HAT, sleeping sickness) and leishmaniasis are neglected tropical diseases (NTDs) which can lead to death of untreated patients
The fusion of the lawsone scaffold with heterocyclic rings such as pyrans can be another promising method in order to obtain new active compounds based on lawsone and various anti-tumor active derivatives as well as tumor cell senescence-inducing complexes were already identified (1e).[26,27]. In continuation of these previous reports, we present new lawsone-derived pyranonaphthoquinone derivatives and their antioxidant and antiparasitic activities against T. brucei, L. major and T. gondii
Summary
Infections of immune-compromised patients and newborn children with the world-wide occurring toxoplasmosis (caused by Toxoplasma gondii parasites) can lead to severe complications and, efficient drugs for the treatment of toxoplasmosis are necessary.[1]. New pyranonaphthoquinone derivatives were synthesized and investigated for their activity against Trypanosoma brucei, Leishmania major, and Toxoplasma gondii parasites. The 3-chloro-4,5-dimethoxyphenyl derivative showed an activity against amastigotes of Leishmania major parasites comparable to that of amphotericin B. The compounds 2a–2o were tested against T. gondii parasites and their activities were compared with those against non-malignant Vero cells (Table 1).
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