Exploiting the Antiparasitic Activity of Naphthalimides Derivatives

Gabriela Cristo^1,2, Luís Gaspar^1,2, Jennifer Noro³, Catarina Baptista^1,2, Paul Kong Thoo-Lin⁴, Maria José Alves³ and Anabela Cordeiro-da-Silva^1,2,5,*
1Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Porto, Portugal
²IBMC-Institute for Molecular and Cell Biology, Parasite Disease Group, Porto, Portugal
³Department of Chemistry, Campus de Gualtar, University of Minho, Braga, Portugal
⁴School of Pharmacy and Life Sciences, Robert Gordon University, Riverside East, Garthdee Road, Aberdeen AB10 1GJ, Scotland;
⁵Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Porto. Portugal

A B S T R A C T
A set of 1,8-naphtalimides derivatives were synthesized and tested against three protozoans that cause important human diseases: Leishmaniainfantum, Trypanosomabrucei and Trypanosomacruzi. Additionally, toxicity was determined by growth inhibition of THP-1 derived macrophages. The results suggest that chemical modifications in the carbon chain linking the naphthalimide and the substituting groups have different effects in the parasites. This work should provide new insights for the design and optimization of more potent and directed naphthalimide derivatives against these organisms.
Keywords: Naphtalimides derivatives, anti-parasitic activity, cytotoxicity.