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1,2,4-Trioxolane and 1,2,4,5-Tetraoxane endoperoxides against old-world Leishma...

Mendes, Andreia; Armada, Ana; Cabral, Lília; Amado, Patrícia; Campino, Lenea; Cristiano, Maria de Lurdes; Cortes, Sofia

Leishmaniasis remains one of the ten Neglected Tropical Diseases with significant morbidity and mortality in humans. Current treatment of visceral leishmaniasis is difficult due to a lack of effective, non-toxic, and non-extensive medications. This study aimed to evaluate the selectivity of 12 synthetic endoperoxides (1,2,4-trioxolanes; 1,2,4,5-tetraoxanes) and uncover their biochemical effects on <i>Leishmania...


Synthesis, structure and antileishmanial evaluation of endoperoxide–pyrazole hy...

Amado, Patrícia S. M.; Costa, Inês C. C.; Paixão, José A.; Mendes, Ricardo F.; Cortes, Sofia; Cristiano, Maria L.

Leishmaniases are among the most impacting neglected tropical diseases. In attempts to repurpose antimalarial drugs or candidates, it was found that selected 1,2,4-trioxanes, 1,2,4,5-tetraoxanes, and pyrazole-containing chemotypes demonstrated activity against <i>Leishmania</i> parasites. This study reports the synthesis and structure of trioxolane–pyrazole (<b>OZ1</b>, <b>OZ2</b>) and tetraoxane–pyrazole (<b>T...


Report of in vitro antileishmanial properties of Iberian macroalgae

Bruno De Sousa, Carolina; Lago, Joao Henrique G.; Macridachis, Jorge; Oliveira, Marta; Fonseca Brito, Luis; Vizetto-Duarte, Catarina; Florindo, Claudia

Here is reported the anti Leishmania infantum activity of 48 hexane, CH2Cl2 and MeOH extracts from 16 macroalgae collected on the Iberian Coast. Seven hexane and CH2Cl2 Cystoseira baccata, Cystoseira barbata, Cystoseira tamariscifolia, Cystoseira usneoides, Dictyota spiralis and Plocamium cartilagineum extracts were active towards promastigotes (IC50 29.8-101.8 mu g/mL) inducing strong morphological alterations...




Report of in vitro antileishmanial properties of Iberian macroalgae

Bruno De Sousa, Carolina; Lago, João Henrique G.; Macridachis, Jorge; Oliveira, Marta; Brito, Luis; Vizetto-Duarte, C; Florindo, Claudia

Here is reported the anti Leishmania infantum activity of 48 hexane, CH2Cl2 and MeOH extracts from 16 macroalgae collected on the Iberian Coast. Seven hexane and CH2Cl2Cystoseira baccata, Cystoseira barbata, Cystoseira tamariscifolia, Cystoseira usneoides, Dictyota spiralis and Plocamium cartilagineum extracts were active towards promastigotes (IC50 29.8-101.8 μg/mL) inducing strong morphological alterations in...


In vitro susceptibility of Leishmania infantum to Artemisinin derivatives and s...

Cortes, Sofia; Albuquerque, Andreia; Cabral, Lília; Lopes, Liliana; Campino, Lenea; Cristiano, Maria L. S.

Leishmaniasis is among the world's most neglected diseases. Currently available drugs for treatment present drawbacks, urging the need for more effective, safer, and cheaper drugs. A small library of artemisinin-derived trioxanes and synthetic trioxolanes was tested against promastigote and intramacrophage amastigote forms of Leishmania infantum. The trioxolanes LC50 and LC95 presented the best activity and saf...


Studies in the mouse model identify strain variability as a major determinant o...

Marques, Filipe; Vale-Costa, Sílvia; Cruz, Tânia; Marques, Joana Moreira; Silva, Tânia; Neves, João Vilares; Cortes, Sofia; Fernandes, Ana

Visceral leishmaniasis is a severe and potentially fatal disease caused by protozoa of the genus Leishmania, transmitted by phlebotomine sandflies. In Europe and the Mediterranean region, L. infantum is the commonest agent of visceral leishmaniasis, causing a wide spectrum of clinical manifestations, including asymptomatic carriage, cutaneous lesions and severe visceral disease. Visceral leishmaniasis is more f...


The first detection of Leishmania major in naturally infected Sergentomyia minu...

Campino, Lenea; Cortes, Sofia; Dionisio, Lidia; Neto, Luis; Afonso, Maria Odete; Maia, Carla

Phlebotomine sandflies of the genus Sergentomyia are widely distributed throughout the Old World. It has been suggested that Sergentomyia spp are involved in the transmission of Leishmania in India and Africa, whereas Phlebotomus spp are thought to be the sole vectors of Leishmania in the Old World. In this study, Leishmania major DNA was detected in one Sergentomyia minuta specimen that was collected in the so...


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