Trypanocidal activity and selectivity in vitro of aromatic amidine compounds upon bloodstream and intracellular forms of Trypanosoma cruzi

dc.creatorSouza, E. M. de
dc.creatorSilva, P. B. da
dc.creatorNefertiti, A. S. G.
dc.creatorIsmail, M. A.
dc.creatorArafa, R. K.
dc.creatorTao, B
dc.creatorNixon-Smith, C. K.
dc.creatorBoykin, D. W.
dc.creatorSoeiro, M. N. C.
dc.date2016-09-22T13:16:06Z
dc.date2016-09-22T13:16:06Z
dc.date2011
dc.date.accessioned2023-09-26T20:23:13Z
dc.date.available2023-09-26T20:23:13Z
dc.identifierSOUZA, E. M. de; et al. Trypanocidal activity and selectivity in vitro of aromatic amidine compounds upon bloodstream and intracellular forms of Trypanosoma cruzi. Experimental Parasitology, v.127, n.2, p.429-435, Feb. 2011.
dc.identifier0014-4894
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/15907
dc.identifier10.1016/j.exppara.2010.10.010
dc.identifier1090-2449
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8855745
dc.descriptionTrypanosoma cruzi is the etiological agent of Chagas disease, an important neglected illness affecting about 12–14 million people in endemic areas of Latin America. The chemotherapy of Chagas disease is quite unsatisfactory mainly due to its poor efficacy especially during the later chronic phase and the considerable well-known side effects. These facts emphasize the need to search for find new drugs. Diamidines and related compounds are minor groove binders of DNA at AT-rich sites and present excellent anti-trypanosomal activity. In the present study, six novel aromatic amidine compounds (arylimidamides and diamidines) were tested in vitro to determine activity against the infective and intracellular stages of T. cruzi, which are responsible for sustaining the infection in the mammalian hosts. In addition, their selectivity and toxicity towards primary cultures of cardiomyocyte were evaluated since these cells represent important targets of infection and inflammation in vivo. The aromatic amidines were active against T. cruzi in vitro, the arylimidamide DB1470 was the most effective compound presenting a submicromolar LD50 values, good selectivity index, and good activity at 4 C in the presence of blood constituents. Our results further justify trypanocidal screening assays with these classes of compounds both in vitro and in vivo in experimental models of T. cruzi infection.
dc.description2030-01-01
dc.formatapplication/pdf
dc.languageeng
dc.publisherElsevier
dc.rightsrestricted access
dc.subjectTrypanosoma cruzi
dc.subjectDoença de Chagas
dc.subjectAtividade tripanocida
dc.subjectAromáticos de amidina
dc.subjectAromatic amidine
dc.subjectTrypanocidal activity
dc.subjectTrypanosoma cruzi
dc.subjectChagas Disease
dc.titleTrypanocidal activity and selectivity in vitro of aromatic amidine compounds upon bloodstream and intracellular forms of Trypanosoma cruzi
dc.typeArticle


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