Design and Synthesis of Cysteine Proteases Inhibitors †
Universitat Jaume I, 12071 Castelló, Spain
†
Presented at the 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery, Barcelona, Spain, 15–17 May 2019.
Proceedings 2019, 22(1), 86; https://doi.org/10.3390/proceedings2019022086
Published: 26 August 2019
(This article belongs to the Proceedings of The 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery)
Cysteine proteases belonging to the papain superfamily have been recognized as interesting therapeutic targets for the search for new drugs against infectious tropical diseases such as malaria (falcipain), Chagas’ disease (curtain), leishmaniasis, and Sleeping sickness (rhodesian), and a number of human pathologies, including cancer, Alzheimer’s disease, and osteoporosis (cathepsins). We have reported irreversible inhibitors Dipeptidyl epoxyesters (kinac/KI up to 92,090 M−1/s−1) [1], Dipeptidyl enoates (kinac/KI up to 1,530,000 M−1/s−1) [2,3], Aminoacyl epoxysulfones [4], and also reversible inhibitors Dipeptidyl nitroalkenes (IC50 up to 0.44 nM) [5] as inhibitors of parasitic cysteine proteases and cathepsins. Inhibition kinetics and computational studies have been used to study the mode of action of these inhibitors.
References
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Gonzalez, F.V. Design and Synthesis of Cysteine Proteases Inhibitors. Proceedings 2019, 22, 86. https://doi.org/10.3390/proceedings2019022086
AMA Style
Gonzalez FV. Design and Synthesis of Cysteine Proteases Inhibitors. Proceedings. 2019; 22(1):86. https://doi.org/10.3390/proceedings2019022086
Chicago/Turabian StyleGonzalez, Florenci V. 2019. "Design and Synthesis of Cysteine Proteases Inhibitors" Proceedings 22, no. 1: 86. https://doi.org/10.3390/proceedings2019022086
