This work describes the synthesis of a series of quaternary ammonium salts and the assessment of their in vitro antileishmanial activity and cytotoxicity. A preliminary discussion on a structure-activity relationship of the compounds is also included. Three series of quaternary ammonium salts were prepared: (i) halomethylated quaternary ammonium salts (series I); (ii) non-halogenated quaternary...

Leishmaniasis represents a serious threat to the health as one of the most important neglected tropical diseases as designated by the World Health Organization. The disease is endemic in 82 countries, among them Tunisia is an indigenous area for cutaneous Leishmaniasis. In a previous work, two tritepenic acids namely oleanolic and maslinic acids have been isolated from olive leaf extract. In th...

Inhibition of Trypanosoma brucei and Leishmania spp. sirtuins has shown promising antiparasitic activity, indicating that these enzymes may be used as targets for drug discovery against trypanosomatid infections. In the present work we carried out a virtual screening focused on the C pocket of Sir2 from Trypanosoma cruzi. Using this approach, the best ligand found was nicotinamide. In vitro tes...

The unlabelled antibody peroxidase-antiperoxidase method was used to study the immunocytochemicalproperties o/Leishmania and Trypanosoma cruzi amastigotes in situ after tissues had been submitted to different fixation procedures. Antisera were obtained from rabbits chronically infected with different strains o f T. cruzi or immunized with L. mexicana amazonensis and L. braziliensis guyanensis, ...

Chagas disease remains one of the most neglected diseases in the world despite being the most important parasitic disease in Latin America. The characteristic chronic manifestation of chagasic cardiomyopathy is the region's leading cause of heart-related illness, causing significant mortality and morbidity. Due to the limited available therapeutic options, new drugs are urgently needed to contr...

BACKGROUND Research in our laboratory has previously shown that immune-mediated transmission blocking may be applied to Leishmania infections and that the LPG molecule and anti-LPG monoclonal antibodies was found to be an excellent candidate against L. major infections. OBJECTIVE To test the effect of monoclonal antibodies (MABs) raised against different species of Leishmania for their abilit...

chalcone (1,3-diarylprop-2-en-1-one) derivatives have been introduced as selective cyclooxygenase-2 inhibitors. in the present study, anti-nociceptive and anti-inflammatory effects of eight novel compounds were evaluated in male mice and wistar rats by using the writhing and formalin-induced paw edema tests respectively. the activities of the compounds were compared with celecoxib as a referenc...

Leishmania spp. must attach to mononuclear phagocyte surfaces before entering this host cell. We investigated the potential role of fibronectin in facilitating parasite attachment. Human plasma fibronectin bound to axenically cultured promastigotes, and promastigotes and amastigotes preferentially bound to fibronectin-coated cover slips. Promastigotes grown in the absence of fibronectin were st...

Development of new therapeutic approach to treat leishmaniasis has become a priority. In the present study, the antileishmanial effect of β-nitrostyrenes was investigated against in vitro promastigotes and amastigotes. A series of β-nitrostyrenes have been synthesized by using Henry reaction and were evaluated for their antimicrobial activities by broth microdilution assay and in vitro antileis...