Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates
Impacte
Scholar |
Altres documents de l'autoria: Royo, Santiago; Schirmeister, Tanja; Kaiser, Marcel; Jung, Sascha; Rodríguez, Santiago; Bautista, José Manuel; González, Florenci
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Mostra el registre complet de l'elementcomunitat-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 |
Metadades
Títol
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoatesAutoria
Data de publicació
2018-09-01Editor
ElsevierISSN
0968-0896Cita bibliogràfica
ROYO, Santiago, et al. Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates. Bioorganic & medicinal chemistry, 2018, vol. 26, no 16, p. 4624-4634.Tipus de document
info:eu-repo/semantics/articleVersió de l'editorial
https://www.sciencedirect.com/science/article/pii/S0968089618308873Versió
info:eu-repo/semantics/publishedVersionParaules clau / Matèries
Resum
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. [-]
Publicat a
Bioorganic & medicinal chemistry, 2018, vol. 26, no 16Proyecto de investigación
Generalitat Valenciana / AICO/2016/32; MINECO / BIO2016-77430R; Generalitat Valenciana under the VALi + d ProgramDrets d'accés
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