Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
ID 4486178
Author(s) Royo, Santiago; Schirmeister, Tanja; Kaiser, Marcel; Jung, Sascha; Rodríguez, Santiago; Bautista, José Manuel; González, Florenci V.
Author(s) at UniBasel Kaiser, Marcel
Year 2018
Title Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates
Journal Bioorganic & medicinal chemistry
Volume 26
Number 16
Pages / Article-Number 4624-4634
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 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 k; 2nd; (M; -1; s; -1; ) values of seven orders of magnitude. In vivo antiprotozoal testing was also performed. Inhibitors exhibited IC; 50; values in the micromolar range against Plasmodium falciparum, Trypanosoma brucei, Trypanosoma cruzi and even more promising lower values against Leishmania donovanii.
Publisher Pergamon
ISSN/ISBN 0968-0896
Full Text on edoc No
Digital Object Identifier DOI 10.1016/j.bmc.2018.07.015
PubMed ID
ISI-Number WOS:000442887900004
Document type (ISI) Journal Article

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