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Natural and Synthetic Naphthoquinones Active Against Trypanosoma Cruzi: An Initial Step Towards New Drugs for Chagas Disease

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Chagas disease is one of the most important endemic diseases in Latin America, caused by Trypanosoma cruzi. The drugs used for the treatment of this disease, nifurtimox and benznidazole, are toxic and present severe side effects. The need of effective drugs, without adverse effects, has stimulated the search for new compounds with potential clinical utility. An overview of a number of natural naphthoquinones tested against T. cruzi parasites is provided. Among natural naphthoquinones, lapachol, β-lapachone and its α-isomer have demonstrated useful trypanocidal activities. In the search for new trypanocidal agents, this review outlines different structural modifications of natural quinones, as well as synthetic quinones, which have been subjected to trypanocidal studies. This review summarizes the mechanism of action and structure-activity relationships of the quinone derivatives, including some theoretical calculations that discuss the correlation of stereo electronic properties with the trypanocidal activity. In this context, this review will be useful for the development of new antichagasic drugs based mainly on structural modification of natural quinones.

Keywords: Chagas disease; Quantitative Structure-Activity Relationships; Sterol biosynthesis; Trypanocidal Activity; Trypanosoma Cruzi; Trypanosoma cruzi; Trypanosomiasis; agranulocytosis; analgesic; anorexia; anti-chagasic drugs; anti-inflammatory; antioxidant; aromatic ring; asymptomatic period; benznidazole; biotransformed; carbonyl groups; cellular respiration; complementary; cytotoxic effects; dermatitis; diarrhea; diospyrin; drug development; electron affinity (EA); electronegativity; electrophilicity; epimastigotes; heterocyclic compounds; human migration; hybridization; hypersensitivity; imidazolic; indazolylquinones; insect's midgut; intestinal colic; lapachol; lapachones; lead compounds; lipophilicity; mammalian organisms; megacolon; megaesophagus; metabolite; morbidity; naphthoimidazoles derivatives; naphthoquinones; nifurtimox; nitrogen substitution; nitroheterocyclic; norlapachones; oxazolic; oxygen radical production; oxygensensitive; parasite; pathology; pharmacokinetic properties; psychic alterations; purine metabolism; quinones; redox cycling; serology; sesquiterpene skeleton; skin manifestations; structure-activity relationships; thrombocytopenic purpura; toxicity; triatomid bugs; trypanocidal activity; trypanocidal effects; tryparedoxins; trypomastigote form; tumor cells; xanthine oxidoreductase; zoonotic infection

Document Type: Research Article


Publication date: January 1, 2011

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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