Sterol biosynthesis inhibitors: Potential chemotherapeutics against chagas disease

Parasitological cure of Chagas disease: is it possible? Is it relevant?

“…2 -Current knowledge seems to indicate that eradication of T. cruzi from infected human patients and animals may be prerequisite to arrest the evolution of the disease and to avert its irreversible long-term consequences (Andrade et al 1991, 1996, Viotti et al 1994, Docampo & Schmuñis 1997, Kaplan et al 1997, Andrade & Zicker 1997, Urbina 1999. Thus, specific chemotherapeutic approaches should play an essential role in the successful clinical outcome of this parasitic disease.…”

“…It is estimated that there are currently >550,000 new cases and 50,000 deaths associated to this condition every year (Docampo & Schmuñis 1997). This disease leads to an annual loss of 2.7 millions of disability adjusted years, being the largest parasitic disease burden in the continent and only third on a global scale after malaria and schistosomiasis (World Bank 1993).…”

In vitro and in vivo activity of amphotericin B-lipid formulations against experimental Trypanosoma cruzi infections.

“…2 Many different classes of drugs have been studied in the search for alternative therapies, 3 and much current interest has focused upon the potential of sterol biosynthesis inhibitors, for example, antifungal azoles. [4][5][6] The polyene antibiotic amphotericin B has previously been shown to have activity in vitro against amastigotes, trypomastigotes, and epimastigotes of T. cruzi, 3 as well as against trypomastigotes at 4ЊC in studies to find new drugs to prevent transmission of Chagas disease by blood transfusion. 7,8 Amphotericin B also exhibited activity against T. cruzi in infected mice, 9 although this was not confirmed in another study.…”

Synthesis of trypanocidal tetrahydrofuran lignans

“…[1][2][3] Approximately 30-40% of the patients are affected by irreversible heart and gastrointestinal tract lesions. 4,5 Thus, such disease has caused approximately 3 million disabilities each year. Therefore, it represents a very serious public health and economic problem in these countries.…”