Antiprotozoal Activity of Triazole Derivatives of Dehydroabietic Acid and Oleanolic Acid

• Main Authors: Mariano Walter Pertino, Celeste Vega, Miriam Rolón, Cathia Coronel, Antonieta Rojas de Arias, Guillermo Schmeda-Hirschmann
• Format: Article
• Language: English
• Published: MDPI AG 2017-02-01
• Series: Molecules
• Subjects: cytotoxicity; dehydroabietic acid; Leishmania spp.; oleanolic acid; triazole derivatives; Trypanosoma cruzi
• Online Access: http://www.mdpi.com/1420-3049/22/3/369

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.