Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates
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Other documents of the author: Royo, Santiago; Schirmeister, Tanja; Kaiser, Marcel; Jung, Sascha; Rodríguez, Santiago; Bautista, José Manuel; González, Florenci
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comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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https://doi.org/10.1016/j.bmc.2018.07.015 |
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Title
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoatesAuthor (s)
Date
2018-09-01Publisher
ElsevierISSN
0968-0896Bibliographic citation
ROYO, Santiago, et al. Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates. Bioorganic & medicinal chemistry, 2018, vol. 26, no 16, p. 4624-4634.Type
info:eu-repo/semantics/articlePublisher version
https://www.sciencedirect.com/science/article/pii/S0968089618308873Version
info:eu-repo/semantics/publishedVersionSubject
Abstract
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. [-]
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Bioorganic & medicinal chemistry, 2018, vol. 26, no 16Investigation project
Generalitat Valenciana / AICO/2016/32; MINECO / BIO2016-77430R; Generalitat Valenciana under the VALi + d ProgramRights
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