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dc.contributor.authorRoyo, Santiago
dc.contributor.authorSchirmeister, Tanja
dc.contributor.authorKaiser, Marcel
dc.contributor.authorJung, Sascha
dc.contributor.authorRodríguez, Santiago
dc.contributor.authorBautista, José Manuel
dc.contributor.authorGonzález, Florenci
dc.date.accessioned2018-11-15T10:58:52Z
dc.date.available2018-11-15T10:58:52Z
dc.date.issued2018-09-01
dc.identifier.citationROYO, Santiago, et al. Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates. Bioorganic & medicinal chemistry, 2018, vol. 26, no 16, p. 4624-4634.ca_CA
dc.identifier.issn0968-0896
dc.identifier.urihttp://hdl.handle.net/10234/177494
dc.description.abstractA family of dipeptidyl enoates has been prepared and tested against the parasitic cysteine proteases rhodesain, cruzain and falcipain-2 related to sleeping sickness, Chagas disease and malaria, respectively. They have also been tested against human cathepsins B and L1 for selectivity. Dipeptidyl enoates resulted to be irreversible inhibitors of these enzymes. Some of the members of the family are very potent inhibitors of parasitic cysteine proteases displaying k2nd (M−1s−1) values of seven orders of magnitude. In vivo antiprotozoal testing was also performed. Inhibitors exhibited IC50 values in the micromolar range against Plasmodium falciparum, Trypanosoma brucei, Trypanosoma cruzi and even more promising lower values against Leishmania donovanii.ca_CA
dc.format.extent11 p.ca_CA
dc.language.isoengca_CA
dc.publisherElsevierca_CA
dc.relation.isPartOfBioorganic & medicinal chemistry, 2018, vol. 26, no 16ca_CA
dc.rights© Elsevier Ltd.ca_CA
dc.subjectinhibitorsca_CA
dc.subjectmalariaca_CA
dc.subjectsleeping sicknessca_CA
dc.subjectchagas diseaseca_CA
dc.subjectcysteine proteasesca_CA
dc.titleAntiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoatesca_CA
dc.typeinfo:eu-repo/semantics/articleca_CA
dc.identifier.doihttps://doi.org/10.1016/j.bmc.2018.07.015
dc.relation.projectIDGeneralitat Valenciana / AICO/2016/32; MINECO / BIO2016-77430R; Generalitat Valenciana under the VALi + d Programca_CA
dc.rights.accessRightsinfo:eu-repo/semantics/restrictedAccessca_CA
dc.relation.publisherVersionhttps://www.sciencedirect.com/science/article/pii/S0968089618308873ca_CA
dc.contributor.funderWe also thank Serveis Centrals d’Instrumentació Científica from Universitat Jaume I for technical support. The authors thank Sabine Maehrlein, Nicole Denk and Ulrike Nowe for performing the enzyme assays, Susana Pérez-Benavente for technical assistance in cytotoxicity and antimalarial assays, Dr. Jochen Kesselring for performing the dialysis and dilution assays, and Patrick Johé for expression and purification of enzymes. S.R. thanks the Generalitat Valenciana for a postdoctoral research grant under theVALi + d Program and the UJI for a postdoctoral researcher position.ca_CA
dc.type.versioninfo:eu-repo/semantics/publishedVersionca_CA


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