• closedAccess   Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates 

      Royo, Santiago; Schirmeister, Tanja; Kaiser, Marcel; Jung, Sascha; Rodríguez, Santiago; Bautista, José Manuel; González, Florenci Elsevier (2018-09-01)
      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 ...
    • closedAccess   Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action 

      Royo Calvo, Santiago; Rodríguez, Santiago; Schirmeister, Tanja; Kesselring, Jochen; Kaiser, Marcel; González, Florenci Wiley (2015-07-14)
      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 ...
    • closedAccess   Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain 

      Latorre, Antonio; Schirmeister, Tanja; Kesselring, Jochen; Jung, Sascha; Johé, Patrick; Hellmich, Ute A.; Heilos, Anna; Engels, Bernd; Krauth-Siegel, R. Luise; Dirdjaja, Natalie; Bou Iserte, Lledó; Rodríguez, Santiago; González, Florenci American Chemical Society (2016)
      Dipeptidyl nitroalkenes are potent reversible inhibitors of cysteine proteases. Inhibitor 11 resulted to be the most potent one with Ki values of 0.49 and 0.44 nM against rhodesain and cruzain, respectively. According to ...