Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates
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Scholar |
Otros documentos de la autoría: Royo, Santiago; Schirmeister, Tanja; Kaiser, Marcel; Jung, Sascha; Rodríguez, Santiago; Bautista, José Manuel; González, Florenci
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Mostrar el registro completo del ítemcomunitat-uji-handle:10234/9
comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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https://doi.org/10.1016/j.bmc.2018.07.015 |
Metadatos
Título
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoatesAutoría
Fecha de publicación
2018-09-01Editor
ElsevierISSN
0968-0896Cita bibliográfica
ROYO, Santiago, et al. Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates. Bioorganic & medicinal chemistry, 2018, vol. 26, no 16, p. 4624-4634.Tipo de documento
info:eu-repo/semantics/articleVersión de la editorial
https://www.sciencedirect.com/science/article/pii/S0968089618308873Versión
info:eu-repo/semantics/publishedVersionPalabras clave / Materias
Resumen
A 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 ... [+]
A 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. [-]
Publicado en
Bioorganic & medicinal chemistry, 2018, vol. 26, no 16Proyecto de investigación
Generalitat Valenciana / AICO/2016/32; MINECO / BIO2016-77430R; Generalitat Valenciana under the VALi + d ProgramDerechos de acceso
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