9Th Brazilian Symposium on Medicinal Chemistry

Leishmaniasis is a parasitic disease that affects more than 100 countries, with 1 million of new cases per year. It's caused by protozoa of the genus Leishmania sp. from more than 20 Leishmania species. Leishmania amazonensis is associated with clinical forms of cutaneous leishmaniasis (CL), including a rare manifestation of CL in human that affects various part of body and makes the treatment difficult. By first-time a serie of Camphor hydrazone derivatives (2a – 2p) was evaluated in vitro against Leishmania amazonensis in extra and intracellular forms. The majority of compounds, displayed activity against the intracellular form, being six active for both forms of the parasite. The compound 2i exhibited the higher activity with value of IC50 (21.78 µM) close to standard miltefosine. All the compounds were non-cytotoxic to macrophages indicating high selectivity. This study indicates the possible development of candidate to leishmanicidal drugs from natural compound of facile access.