dc.creatorBollini, Mariela
dc.creatorBruno, Ana Maria
dc.creatorNiño, Maria Eugenia
dc.creatorCasal, Juan José
dc.creatorSasiambarrena, Leandro Daniel
dc.creatorGonzález Valdez, Damián Ariel
dc.creatorBattini, Leandro
dc.creatorPuente, Vanesa Rocío
dc.creatorLombardo, Maria Elisa
dc.date.accessioned2019-11-07T21:13:25Z
dc.date.accessioned2022-10-15T07:09:52Z
dc.date.available2019-11-07T21:13:25Z
dc.date.available2022-10-15T07:09:52Z
dc.date.created2019-11-07T21:13:25Z
dc.date.issued2018-10
dc.identifierBollini, Mariela; Bruno, Ana Maria; Niño, Maria Eugenia; Casal, Juan José; Sasiambarrena, Leandro Daniel; et al.; Synthesis, 2D-QSAR studies and biological evaluation of quinazoline derivatives as potent anti-trypanosoma cruzi agents; Bentham Science Publishers; Medicinal Chemistry; 14; 10-2018; 1-12
dc.identifier1573-4064
dc.identifierhttp://hdl.handle.net/11336/88254
dc.identifierCONICET Digital
dc.identifierCONICET
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/4358888
dc.description.abstractBackground: Chagas disease affects about 7 million people worldwide. Only two drugs are currently available for the treatment for this parasite disease, namely, benznidazol (Bzn) and nifurtimox (Nfx). Both drugs have limited curative power in the chronic phase of the disease. Therefore, continuous research is an urgent need so as to discover novel therapeutic alternatives. Objective: The development of safer and more efficient therapeutic anti-T. cruzi drugs continues to be a major goal in trypanocidal chemotherapy. Method: Synthesis, 2D-QSAR and drug-like physicochemical properties of a set of quinazolinone and quinazoline derivatives were studied as trypanocidal agents. All compounds were screened in vitro against Trypanosoma cruzi (Tulahuen strain, Tul 2 stock) epimastigotes and bloodstream trypomastigotes. Results: Out of 34 compounds synthesized and tested, six compounds (5a, 5b, 9b, 9h, 13f and 13p) displayed significant activity against both epimastigotes and tripomastigotes, without exerting toxicity on Vero cells. Conclusion: The antiprotozoal activity of these quinazolinone and quinazoline derivatives represents an interesting starting point for a medicinal chemistry program aiming at the development of novel chemotherapies for Chagas disease
dc.languageeng
dc.publisherBentham Science Publishers
dc.relationinfo:eu-repo/semantics/altIdentifier/url/http://www.eurekaselect.com/165997/article
dc.relationinfo:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.2174/1573406414666181005145042
dc.rightshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.subjectChagas disease
dc.subjectquinazolines derivatives
dc.subjectQSAR
dc.subjectTrypanosoma cruzi
dc.titleSynthesis, 2D-QSAR studies and biological evaluation of quinazoline derivatives as potent anti-trypanosoma cruzi agents
dc.typeinfo:eu-repo/semantics/article
dc.typeinfo:ar-repo/semantics/artículo
dc.typeinfo:eu-repo/semantics/publishedVersion


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