Abstract
Tropical parasitic diseases such as Chagas disease and leishmaniasis are considered a major public health problem affecting hundreds of millions of people worldwide. As the drugs currently used to treat these diseases have several disadvantages and side effects, there is an urgent need for new drugs with better selectivity and less toxicity. Structural modifications of naturally occurring and synthetic compounds using click chemistry have enabled access to derivatives with promising antiparasitic activity. The antiprotozoal activity of the terpenes dehydroabietic acid, dehydroabietinol, oleanolic acid, and 34 synthetic derivatives were evaluated against epimastigote forms of Trypanosoma cruzi and promastigotes of Leishmaniabraziliensis and Leishmania infantum. The cytotoxicity of the compounds was assessed on NCTC-Clone 929 cells. The activity of the compounds was moderate and the antiparasitic effect was associated with the linker length between the diterpene and the triazole in dehydroabietinol derivatives. For the oleanolic acid derivatives, a free carboxylic acid function led to better antiparasitic activity.
Highlights
Chagas is endemic in 21 countries in Latin America
It was estimated that 90–100 million people are at risk of contracting Chagas disease and eight million are infected by the flagellate protozoan Trypanosoma cruzi with approximately 12,000 deaths and 56,000 new cases per year [5]
34 terpene-triazole derivatives were synthesized starting from the natural products dehydroabietic acid, dehydroabietinol, and oleanolic acid
Summary
Chagas is endemic in 21 countries in Latin America It is a zoonotic parasitosis considered one of the most important neglected diseases in Latin America with a total of 520,043 DALYs (years of disability-adjusted life) [1,2,3,4]. It was estimated that 90–100 million people are at risk of contracting Chagas disease and eight million are infected by the flagellate protozoan Trypanosoma cruzi with approximately 12,000 deaths and 56,000 new cases per year [5]. An estimated 5.4 million people will develop cardiac Chagas disease [1,6], while 900,000 will have megaesophagus and megacolon [1]. More than two million people infected with Chagas disease live in Spain and other European countries [7], and even in other continents [8]
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