4.4 Review

Natural and Synthetic Naphthoquinones as Potential Anti-Infective Agents

Journal

CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 21, Issue 22, Pages 2046-2069

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026621666210915121348

Keywords

Naphthoquinones; Leishmania spp; Trypanosoma cruzi; Plasmodium falciparum; Toxoplasma gondii; Toxocara canis

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Naphthoquinones are aromatic compounds with antibacterial, antifungal, and antiprotozoal properties, which can be obtained from both natural and synthetic sources. Research on naphthoquinones and their derivatives contributes to the development of new chemotherapeutic agents against parasitic diseases.
Background: Naphthoquinones are a class of aromatic compounds relevant for their chemical characteristics, structural properties, and biological activity. These compounds are found in nature with a wide range of effects, highlighting their antibacterial, antifungal, and antiprotozoal properties. Additionally, naphthoquinones are used as a scaffold to obtain new derivatives with pharmacological potential, mainly compounds against parasitic diseases. Objective: The purpose of this work was to carry out a comprehensive review of naphthoquinones and their derivatives obtained from both natural and synthetic sources, also, to analyze their biological activity against Leishmania spp. (Leishmaniasis), Trypanosoma cruzi (Chagas disease), Plasmodium falciparum (Malaria), Toxoplasma gondii (Toxoplasmosis), and Toxocara canis (Toxocariasis). All of these agents are responsible for relevant diseases worldwide. Results: Natural naphthoquinones, such as plumbagin, diospyrin, burmanin, lapachol, lawsone and psychorubrin, show an antiprotozoal activity similar or enhanced antiprotozoal activity to reference drugs. Some naphthoquinones obtained by synthesis or semi-synthesis showed better biological activity or less toxic effects than natural compounds. Conclusion: In this review, natural and synthetic naphthoquinones showed antiparasitic activity, in most cases, with improved results than current drugs currently used in clinical trials. A modification of their structure with different functional groups can enhance their biological effects, improve solubility, and reduce undesirable side effects. Therefore, naphthoquinones are important molecules in the development of new chemotherapeutic agents against parasitic diseases.

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