0000000000234228

AUTHOR

David Gomez-herrera

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In vitro activity of scorpiand-like azamacrocycle derivatives in promastigotes and intracellular amastigotes of Leishmania infantum and Leishmania br…

2012

The activity of a family scorpiand-like azamacrocycles against Leishmania infantum and Leishmania braziliensis was studied using promastigotes, axenic and intracellular amastigotes forms. All the compounds are more active and less toxic than meglumine antimoniate (Glucantime). Moreover, the data on infection rates and amastigotes showed that compounds P2Py, PN and P3Py are the most active against both species of Leishmania. On the other hand, studies on the inhibitory effect of these compounds on SOD enzymes showed that while the inhibition of the Fe-SOD enzyme of the promastigote forms of the parasites is remarkable, the inhibition of human CuZn-SOD and Mn-SOD from Escherichia coli is negl…

Macrocyclic CompoundsMeglumine antimoniateAntiprotozoal AgentsLeishmania braziliensisMicrobiologyStructure-Activity RelationshipParasitic Sensitivity TestsDrug DiscoverymedicineLeishmania infantumAmastigoteAxenicPharmacologychemistry.chemical_classificationAza CompoundsbiologyDose-Response Relationship DrugMolecular StructureOrganic ChemistryGeneral MedicineLeishmaniabiology.organism_classificationLeishmania braziliensisEnzymechemistryLeishmania infantumIntracellularmedicine.drugEuropean journal of medicinal chemistry
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