Sistema FMUSP-HC: Faculdade de Medicina da Universidade de São Paulo (FMUSP) e Hospital das Clínicas da FMUSPSILVA, Simone Carolina Soares Petri ePALACE-BERL, FannyTAVARES, Leoberto CostaSOARES, Sandra Regina CastroLINDOSO, Jose Angelo Lauletta2016-07-182016-07-182016EXPERIMENTAL PARASITOLOGY, v.163, p.68-75, 20160014-4894https://observatorio.fm.usp.br/handle/OPI/14585Leishmaniasis is an overlooked tropical disease affecting approximately 1 million people in several countries. Clinical manifestation depends on the interaction between Leishmania and the host's immune response. Currently available treatment options for leishmaniasis are limited and induce severe side effects. In this research, we tested nitro-heterocyclic compounds (BSF series) as a new alternative against Leishmania. Its activity was measured in Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes using MIT colorimetric assay. Additionally, we assessed the phosphatidylserine exposure by promastigotes, measured by flow cytometry, as well as nitric oxide production, measured by Griess' method. The nitro-heterocyclic compounds (BSF series) showed activity against L. (L.) infantum promastigotes, inducting the phosphatidylserine exposition by promastigotes, decreasing intracellular amastigotes and increasing oxide nitric production. The selectivity index was more prominent to Leishmania than to macrophages. Compared to amphotericin b, our compounds presented higher IC50, however the selectivity index was more specific to parasite than to amphotericin b. In conclusion, these nitro-heterocyclic compounds showed to be promising as an anti-Leishmania drug, in in vitro studies.engrestrictedAccessLeishmania (L.) infantumNitroheterocyclic compoundsTHP-1 cellsNitric oxideApoptosistrypanosoma-cruzitrypanothione reductasechagas-diseaselipoamide dehydrogenasebioactivity evaluationamphotericin-bcytotoxicitychemotherapyamazonensistargetsarticleCopyright ACADEMIC PRESS INC ELSEVIER SCIENCE10.1016/j.exppara.2016.01.007Parasitology1090-2449