Design and Synthesis of Cysteine Protease Inhibitors †
Department de Química Inorgànica i Orgànica, Universitat Jaume I, 12071 Castelló, Spain
†
Presented at the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain, 8 September 2017.
Proceedings 2017, 1(6), 672; https://doi.org/10.3390/proceedings1060672
Published: 18 October 2017
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
We have been preparing new dipeptidyl inhibitors against parasitic cysteine proteases cruzain (related to Chagas disease) and rhodesain (related to Sleeping Sickness disease), and against human cathepsins. Inhibitors display new warheads embedded into a dipeptidic framework. Dipeptidyl epoxyesters [1] and Dipeptidyl enoates [2] are highly potent irreversible inhibitors of cruzain and rhodesain. We also prepared an oxidized version of well-known Vinylsulfones (Epoxysulfones [3]) as inhibitors of human cathepsins. Recently, we have reported the synthesis of Dipeptidyl nitroalkenes [4] as a new type of highly potent covalent reversible inhibitors of cysteine proteases exhibiting certain selectivity for the parasitic cysteine proteases rhodesain and cruzain.
Acknowledgments
The author thanks Generalitat Valenciana (AICO/2016/32) for financial support.
Conflicts of Interest
The author declares no conflict of interest.
References
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Gonzalez, F.V. Design and Synthesis of Cysteine Protease Inhibitors. Proceedings 2017, 1, 672. https://doi.org/10.3390/proceedings1060672
AMA Style
Gonzalez FV. Design and Synthesis of Cysteine Protease Inhibitors. Proceedings. 2017; 1(6):672. https://doi.org/10.3390/proceedings1060672
Chicago/Turabian StyleGonzalez, Florenci V. 2017. "Design and Synthesis of Cysteine Protease Inhibitors" Proceedings 1, no. 6: 672. https://doi.org/10.3390/proceedings1060672
