@misc{10481/101082, year = {2013}, url = {https://hdl.handle.net/10481/101082}, abstract = {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 negligible. The ultrastructural alterations observed in treated promastigote forms confirmed that the compounds having the highest activity were those causing the largest cell damage. The modifications observed by (1)H NMR, and the amounts of catabolites excreted by the parasites after treatment with the compounds, suggested that the catabolic mechanism could depend on the structure of the side chains linked to the aza-scorpiand macrocycles.}, organization = {Ministerio de Ciencia e Innovación and FEDER funds of the E.U. (Projects CTQ2009-14288-CO4-01 and CONSOLIDER INGENIO 2010 CSD2010-00065), Generalitat Valenciana (PROMETEO 2011/008)}, title = {In vitro activity of scorpiand-like azamacrocycle derivatives in promastigotes and intracellular amastigotes of Leishmania infantum and Leishmania braziliensis}, doi = {10.1016/j.ejmech.2013.01.001}, author = {Marín Sánchez, Clotilde and Clares, M. Paz and Ramírez-Macías, Inmaculada and Blasco, Salvador and Olmo, Francisco and Soriano, Conxa and Verdejo, Begoña and Rosales Lombardo, María José and Gomez-Herrera, David and García-España, Enrique and Sánchez Moreno, Manuel}, }