Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.

Bioorganic & Medicinal Chemistry Letters
Jeremy P MallariR Kiplin Guy

Abstract

Human African trypanosomiasis (HAT) is caused by the protozoan parasite Trypanosoma brucei. The cysteine proteases of T. brucei have been shown to be crucial for parasite replication and represent an attractive point for therapeutic intervention. Herein we describe the synthesis of a series of thiosemicarbazones and their activity against the trypanosomal cathepsins TbcatB and rhodesain, as well as human cathepsins L and B. The activity of these compounds was determined against cultured T. brucei, and specificity was assessed with a panel of four mammalian cell lines.

References

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Citations

Oct 30, 2009·Expert Reviews in Molecular Medicine·Shane R Wilkinson, John M Kelly
Apr 25, 2013·Journal of Medicinal Chemistry·Roberta EttariPaola Conti
Sep 23, 2009·Journal of Medicinal Chemistry·Jeremy P MallariR Kiplin Guy
Jul 18, 2012·PLoS Neglected Tropical Diseases·Jon J VermeireConor R Caffrey
Oct 23, 2013·Future Medicinal Chemistry·Lori FerrinsJonathan B Baell
May 3, 2012·International Journal for Parasitology·Dietmar SteverdingConor R Caffrey
Mar 8, 2016·The Journal of Organic Chemistry·Hongxiang WuZhuo Zeng
Jan 12, 2012·Biochimica Et Biophysica Acta·Tatiana F R CostaAna Paula C A Lima
May 5, 2009·Molecular and Biochemical Parasitology·Conor R Caffrey, Dietmar Steverding
Sep 24, 2011·Experimental Parasitology·Renata O A SoaresLeonor L Leon
Sep 3, 2014·The American Journal of Chinese Medicine·Nguyen Huu TungYukihiro Shoyama
May 19, 2009·Bioorganic & Medicinal Chemistry Letters·Jeremy P MallariR Kiplin Guy
Aug 4, 2012·Organic & Biomolecular Chemistry·Giuseppina ChianeseOrazio Taglialatela-Scafati
Feb 12, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Dibyendu Dana, Sanjai K Pathak
Oct 12, 2010·Bioorganic & Medicinal Chemistry Letters·G D Kishore KumarKevin G Pinney
Mar 20, 2010·Journal of Natural Products·Yunjiang FengRonald J Quinn
Dec 12, 2018·Journal of Chemical Information and Modeling·Lucianna H SantosRafaela S Ferreira
May 4, 2010·European Journal of Medicinal Chemistry·Roberta EttariSilvana Grasso

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African Trypanosomiasis

African trypanosomiasis, also known as sleeping sickness, is an insect-borne parasitic disease of humans and other animals. It is caused by protozoa of the species Trypanosoma brucei and almost invariably progresses to death unless treated. Discover the latest research on African trypanosomiasis here.