dc.creatorRobledo Restrepo, Sara María
dc.creatorMartínez Martínez, Alejandro
dc.creatorGaleano Jaramillo, Elkin de Jesús
dc.creatorSurmay Surmay, Verónica
dc.creatorPastrana Restrepo, Manuel Humberto
dc.date2023-04-07T17:52:19Z
dc.date2023-04-07T17:52:19Z
dc.date2019
dc.date.accessioned2024-04-23T17:49:49Z
dc.date.available2024-04-23T17:49:49Z
dc.identifier0103-5053
dc.identifierhttps://hdl.handle.net/10495/34533
dc.identifier10.21577/0103-5053.20180160
dc.identifier1678-4790
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/9229948
dc.descriptionABSTRACT: Novel iodotyramides with para-substituted benzoic acids were synthesized via electrophilic aromatic substitutions and amide coupling via N,N’-diisopropylcarbodiimide (DIC) in dimethylformamide (DMF). All derivatives were in vitro screened against U-937 macrophages and Plasmodium falciparum, Leishmania panamensis and Trypanosoma cruzi protozoan parasites. The hemolytic activity was evaluated on human red blood cells (RBC). Compounds N-(4-hydroxy-3,5-diiodophenethyl)-4-methylbenzamide and N-(3,5-diiodo4-methoxyphenethyl)-4-methoxybenzamide were the most active against L. panamensis with an effective concentration 50 (EC50) of 17.9 and 17.5 μg mL-1, respectively; while compounds N-(3,5-diiodo-4-methoxyphenethyl)-4-methylbenzamide and N-(3,5-diiodo-4-methoxyphenethyl)- 4-methoxybenzamide were the most active for T. cruzi with EC50 values of 23.75 and 6.19 μg mL-1 , respectively. In contrast, all derivatives showed high activity against P. falciparum with EC50 < 25 μg mL-1, except compound N-(4-hydroxy-3,5-diiodophenethyl)-benzamide. No compound was hemolytic over RBC. This report represents the importance of novel iodotyramides as anti-parasites agents.
dc.descriptionCOL0015099
dc.descriptionCOL0015043
dc.format8
dc.formatapplication/pdf
dc.formatapplication/pdf
dc.languageeng
dc.publisherSociedade Brasileira de Química
dc.publisherProductos Naturales Marinos
dc.publisherPrograma de Estudio y Control de Enfermedades Tropicales (PECET)
dc.publisherSão Paulo, Brasil
dc.relationJ. Braz. Chem. Soc.
dc.rightsinfo:eu-repo/semantics/openAccess
dc.rightshttp://creativecommons.org/licenses/by-nc-nd/2.5/co/
dc.rightshttp://purl.org/coar/access_right/c_abf2
dc.rightshttps://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subjectAnticuerpos Antiprotozoarios
dc.subjectAntibodies, Protozoan
dc.subjectLeishmania guyanensis
dc.subjectPlasmodium falciparum
dc.subjectTrypanosoma cruzi
dc.subjectCitotoxicidad
dc.subjectCytotoxicity
dc.subjecthttp://aims.fao.org/aos/agrovoc/c_34251
dc.titleAnti-parasite activity of novel 3,5-diiodophenethyl-benzimides
dc.typeinfo:eu-repo/semantics/article
dc.typeinfo:eu-repo/semantics/publishedVersion
dc.typehttp://purl.org/coar/resource_type/c_2df8fbb1
dc.typehttps://purl.org/redcol/resource_type/ART
dc.typeArtículo de investigación


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