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Please use this identifier to cite or link to this item: http://acervodigital.unesp.br/handle/11449/113468
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dc.contributor.authorAlvarez, Guzman-
dc.contributor.authorVarela, Javier-
dc.contributor.authorMarquez, Pablo-
dc.contributor.authorGabay, Martin-
dc.contributor.authorArias Rivas, Carmen Elena-
dc.contributor.authorCuchilla, Karina-
dc.contributor.authorEcheverria, Gustavo A.-
dc.contributor.authorPiro, Oscar E.-
dc.contributor.authorChorilli, Marlus-
dc.contributor.authorLeal, Sandra M.-
dc.contributor.authorEscobar, Patricia-
dc.contributor.authorSerna, Elva-
dc.contributor.authorTorres, Susana-
dc.contributor.authorYaluff, Gloria-
dc.contributor.authorVera de Bilbao, Ninfa I.-
dc.contributor.authorGonzalez, Mercedes-
dc.contributor.authorCerecetto, Hugo-
dc.date.accessioned2014-12-03T13:11:43Z-
dc.date.accessioned2016-10-25T20:14:57Z-
dc.date.available2014-12-03T13:11:43Z-
dc.date.available2016-10-25T20:14:57Z-
dc.date.issued2014-05-22-
dc.identifierhttp://dx.doi.org/10.1021/jm500018m-
dc.identifier.citationJournal Of Medicinal Chemistry. Washington: Amer Chemical Soc, v. 57, n. 10, p. 3984-3999, 2014.-
dc.identifier.issn0022-2623-
dc.identifier.urihttp://hdl.handle.net/11449/113468-
dc.identifier.urihttp://acervodigital.unesp.br/handle/11449/113468-
dc.description.abstractChagas disease, caused by Trypanosoma cruzi parasite, was described thousands of years ago. Currently, it affects millions of people, mostly in Latin America, and there are not suitable drugs for treating it. As an attempt to find appropriate drugs to deal with this problem, we report here on the design, synthesis, and characterization of 82 new compounds. Trypanosomicidal behavior in vitro showed more than 20 outstanding derivatives with anti-Trypanosoma cruzi activity. Furthermore, we studied the nonspecific toxicity against mammalian cells determining their selectivity and also performed mutagenicity studies. Proof of concept, in vivo studies, was conducted with two of the most promising derivatives (77 and 80). They were identified as candidates because they have (i) very simple and cost-effective syntheses; (ii) activity against different stages and strains of the parasite showing excellent in vivo behavior during the acute phase of Chagas disease; and (iii) neither nonspecific toxicity nor mutagenic activity.en
dc.description.sponsorshipIberoamerican Program for Science and Technology (CYTED)-
dc.description.sponsorshipnetwork RIDIMEDCHAG-
dc.description.sponsorshipViceministerio de Ciencia y Tecnologia (El Salvador)-
dc.description.sponsorshipAgenda Uruguaya de Cooperacion Internacional (Uruguay)-
dc.description.sponsorshipANII (Uruguay)-
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)-
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
dc.description.sponsorshipPrograma de Apoio ao Desenvolvimento Cientifico (PADC-FCF-UNESP)-
dc.format.extent3984-3999-
dc.language.isoeng-
dc.publisherAmer Chemical Soc-
dc.sourceWeb of Science-
dc.titleOptimization of Antitrypanosomatid Agents: Identification of Nonmutagenic Drug Candidates with in Vivo Activityen
dc.typeoutro-
dc.contributor.institutionUniv Republica-
dc.contributor.institutionCtr Nacl Invest Cient El Salvador-
dc.contributor.institutionUniv Nacl La Plata-
dc.contributor.institutionConsejo Nacl Invest Cient & Tecn-
dc.contributor.institutionUniversidade Estadual Paulista (UNESP)-
dc.contributor.institutionUniv Ind Santander-
dc.contributor.institutionUniv Nacl Asuncion-
dc.description.affiliationUniv Republica, Grp Quim Med, Lab Quim Organ, Fac Ciencias,Fac Quim, Montevideo 11400, Uruguay-
dc.description.affiliationCtr Nacl Invest Cient El Salvador, San Salvador, El Salvador-
dc.description.affiliationUniv Nacl La Plata, Fac Ciencias Exactas, Dept Fis, RA-1900 La Plata, Buenos Aires, Argentina-
dc.description.affiliationConsejo Nacl Invest Cient & Tecn, Inst IFLP, CCT La Plata, RA-1900 La Plata, Buenos Aires, Argentina-
dc.description.affiliationUNESP, Sch Pharmaceut Sci, Dept Drugs & Pharmaceut, Araraquara, Brazil-
dc.description.affiliationUniv Ind Santander, Dept Ciencias Basicas, Ctr Invest Enfermedades Tropicales, Bucaramanga, Colombia-
dc.description.affiliationUniv Nacl Asuncion, Inst Ciencias Salud, Dept Med Trop, Asuncion, Paraguay-
dc.description.affiliationUnespUNESP, Sch Pharmaceut Sci, Dept Drugs & Pharmaceut, Araraquara, Brazil-
dc.identifier.doi10.1021/jm500018m-
dc.identifier.wosWOS:000336510100006-
dc.rights.accessRightsAcesso restrito-
dc.relation.ispartofJournal of Medicinal Chemistry-
Appears in Collections:Artigos, TCCs, Teses e Dissertações da Unesp

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