The evaluation of quinonoid compounds against Trypanosoma cruzi: synthesis of imidazolic anthraquinones, nor-beta-lapachone derivatives and beta-lapachone-based 1,2,3-triazoles

dc.creatorSilva, Eufrânio N. da
dc.creatorGuimarães, Tiago T.
dc.creatorMenna-Barreto, Rubem F. S.
dc.creatorPinto, Maria do Carmo F. R.
dc.creatorSimone, Carlos A. de
dc.creatorPessoa, Claudia
dc.creatorCavalcanti, Bruno C.
dc.creatorSabino, José R.
dc.creatorAndrade, Carlos Kleber Z.
dc.creatorGoulart, Marilia O. F.
dc.creatorCastro, Solange L. de
dc.creatorPinto, Antônio V.
dc.date2018-11-29T14:22:28Z
dc.date2018-11-29T14:22:28Z
dc.date2010
dc.date.accessioned2023-09-26T23:01:34Z
dc.date.available2023-09-26T23:01:34Z
dc.identifierSILVA JÚNIOR, Eufrânio N. da; et al. The evaluation of quinonoid compounds against Trypanosoma cruzi: Synthesis of imidazolic anthraquinones, nor-b-lapachone derivatives and b-lapachone-based 1,2,3-triazoles. Bioorganic & Medicinal Chemistry, v.18, p.3224–3230, 2010.
dc.identifier0968-0896
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/30319
dc.identifier10.1016/j.bmc.2010.03.029
dc.identifier1464-3391
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8885981
dc.descriptionIn continuing our screening program of naphthoquinone activity against Trypanosoma cruzi, the aetiological agent of Chagas' disease, new beta-lapachone-based 1,2,3-triazoles, 3-arylamino-nor-beta-lapachones, 3-alkoxy-nor-beta-lapachones and imidazole anthraquinones were synthesised and evaluated against bloodstream trypomastigote forms of the parasite. Compounds 2,2-dimethyl-3-(2,4-dibromophenylamino)-2,3-dihydro-naphtho[1,2-b]furan-4,5-dione, IC(50)/24h 24.9+/-7.4 and 4-azido-3-bromo-2,2-dimethyl-3,4-dihydro-2H-benzo[h]chromene-5,6-dione with 23.4+/-3.8 microM showed a trypanosomicidal activity higher than benznidazole. These results demonstrate the potential of naphthoquinone derivatives as novel structures for the development of alternative drugs for Chagas' disease.
dc.description2030-01-01
dc.formatapplication/pdf
dc.languageeng
dc.publisherElsevier
dc.rightsrestricted access
dc.subjectDoença de Chagas
dc.subjectTrypanosoma cruzi
dc.subjectQuimioterapia experimental
dc.subjectNaftoquinonas
dc.subjectNaphthoquinones
dc.subjectNor-b-lapachone
dc.subjectChagas Disease
dc.subjectTrypanosoma cruzi
dc.subjectExperimental chemotherapy
dc.subjectNaftoquinonas
dc.titleThe evaluation of quinonoid compounds against Trypanosoma cruzi: synthesis of imidazolic anthraquinones, nor-beta-lapachone derivatives and beta-lapachone-based 1,2,3-triazoles
dc.typeArticle


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