1000981-20-3Relevant academic research and scientific papers
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates
Royo, Santiago,Schirmeister, Tanja,Kaiser, Marcel,Jung, Sascha,Rodríguez, Santiago,Bautista, José Manuel,González, Florenci V.
, p. 4624 - 4634 (2018/07/25)
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.
Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action
Royo, Santiago,Rodríguez, Santiago,Schirmeister, Tanja,Kesselring, Jochen,Kaiser, Marcel,González, Florenci V.
supporting information, p. 1484 - 1487 (2015/09/07)
Dipeptidyl enoates were prepared through a high-yielding two-step synthetic route. They have a dipeptidic structure with a 4-oxoenoate moiety as a warhead with multiple reactive sites. Dipeptidyl enoates were screened against rhodesain and human cathepsin
CYSTEINE PROTEASES INHIBITORS
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Page/Page column 11, (2010/04/25)
Substantially pure diastereoisomeric compounds of formula Ia, alternatively Ib, or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, including hydrates, wherein PG is a protective group; R1 is a radica
Dipeptidyl-α,β-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain
Gonzalez, Florenci V.,Izquierdo, Javier,Rodriguez, Santiago,McKerrow, James H.,Hansell, Elizabeth
, p. 6697 - 6700 (2008/09/17)
The dipeptidyl epoxyesters 3 and 4 are potent, irreversible inhibitors of cruzain and rhodesain.
