Mostrar el registro sencillo del ítem

dc.contributor.authorOtero, Elver
dc.contributor.authorGarcía, Elisa
dc.contributor.authorPalacios, Génesis
dc.contributor.authorYepes, Lina M.
dc.contributor.authorCarda, Miguel
dc.contributor.authorAgut, Raúl
dc.contributor.authorVélez, Iván D.
dc.contributor.authorCardona Galeano, Wilson Isidro
dc.contributor.authorRobledo, Sara M.
dc.date.accessioned2017-11-15T10:26:09Z
dc.date.available2017-11-15T10:26:09Z
dc.date.issued2017-09-29
dc.identifier.citationOTERO, Elver; GARCÍA, Elisa; PALACIOS, Génesis; YEPES, Lina M.; CARDA USÓ, Miguel; AGUT, Raúl; VÉLEZ, Ivan D.; CARDONA, Wilson; ROBLEDO, Sara M. Triclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activities. European Journal of Medicinal Chemistry (2017), v. 141, p. 73-83ca_CA
dc.identifier.urihttp://hdl.handle.net/10234/170055
dc.description.abstractThe synthesis, cytotoxicity, anti-leishmanial and anti-trypanosomal activities of twelve triclosan-caffeic acid hybrids are described herein. The structure of the synthesized products was elucidated by a com- bination of spectrometric analyses. The synthesized compounds were evaluated against amastigotes forms of L. (V) panamensis , which is the most prevalent Leishmania species in Colombia, and against Trypanosoma cruzi, which is the pathogenic species to humans. Cytotoxicity was evaluated against hu- man U-937 macrophages. Eight compounds were active against L. (V) panamensis ( 18 e 23, 26 and 30 ) and eight of them against T. cruzi ( 19 e 22 , 24 and 28 e 30 ) with EC 50 values lower than 40 m M. Compounds 19 e 22 , 24 and 28 e 30 showed higher activities than benznidazole (BNZ). Esters 19 and 21 were the most active compounds for both L. (V) panamensis and T. cruzi with 3.82 and 11.65 m M and 8.25 and 8.69 m M, respectively. Compounds 19 e 22 , 24 and 28 e 30 showed higher activities than benznidazole (BNZ). Most of the compounds showed antiprotozoal activity and with exception of 18 , 26 and 28 , the remaining compounds were toxic for mammalian cells, yet they have potential to be considered as candidates for anti-trypanosomal and anti-leishmanial drug development. The activity is dependent on the length of the alkyl linker with compound 19 , bearing a four-carbon alkyl chain, the most performing hybrid. In general, hydroxyl groups increase both activity and cytotoxicity and the presence of the double bond in the side chain is not decisive for cytotoxicity and anti-protozoal activity.ca_CA
dc.format.extent27 p.ca_CA
dc.format.mimetypeapplication/pdfca_CA
dc.language.isoengca_CA
dc.publisherElsevierca_CA
dc.relation.isPartOfEuropean Journal of Medicinal Chemistry (2017), v. 141ca_CA
dc.rights.urihttp://rightsstatements.org/vocab/CNE/1.0/*
dc.subjectLeishmaniasisca_CA
dc.subjectChagas diseaseca_CA
dc.subjectTrypanosoma cruzica_CA
dc.subjectAntiprotozoal activityca_CA
dc.subjectCytotoxicityca_CA
dc.subjectTriclosanca_CA
dc.subjectCaffeic acidca_CA
dc.subjectHybridsca_CA
dc.titleTriclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activitiesca_CA
dc.typeinfo:eu-repo/semantics/articleca_CA
dc.identifier.doihttps://doi.org/10.1016/j.ejmech.2017.09.064
dc.relation.projectIDOLCIENCIAS (Grant No. 0333 e 2013, code: 111556933423) and Universidad de Antioquia for financial support.ca_CA
dc.rights.accessRightsinfo:eu-repo/semantics/openAccessca_CA
dc.relation.publisherVersionhttp://www.sciencedirect.com/science/article/pii/S0223523417307791?via%3Dihubca_CA
dc.type.versioninfo:eu-repo/semantics/submittedVersionca_CA


Ficheros en el ítem

Thumbnail

Este ítem aparece en la(s) siguiente(s) colección(ones)

Mostrar el registro sencillo del ítem