The Inhibition of Cysteine Proteases Rhodesain and TbCatB: A Valuable Approach to Treat Human African Trypanosomiasis

2016 ◽  
Vol 16 (17) ◽  
pp. 1374-1391 ◽  
Author(s):  
Roberta Ettari ◽  
Santo Previti ◽  
Lucia Tamborini ◽  
Gregorio Cullia ◽  
Silvana Grasso ◽  
...  
Keyword(s):  
Human African Trypanosomiasis ◽  
Cysteine Proteases ◽  
African Trypanosomiasis

scholarly journals Benzimidazole inhibitors of the major cysteine protease of Trypanosoma brucei

2019 ◽  
Vol 11 (13) ◽  
pp. 1537-1551 ◽  
Author(s):  
Glaécia AN Pereira ◽  
Lucianna H Santos ◽  
Steven C Wang ◽  
Luan C Martins ◽  
Filipe S Villela ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Human African Trypanosomiasis ◽  
Cysteine Proteases ◽  
African Trypanosomiasis ◽  
High Similarity ◽  
Trypanosoma Brucei Brucei ◽  
Structure Activity ◽  
Starting Point ◽  
Competitive Inhibitors ◽  
Enzyme Selectivity

Aim: Limitations in available therapies for trypanosomiases indicate the need for improved medicines. Cysteine proteases cruzain and rhodesain are validated targets for treatment of Chagas disease and human African trypanosomiasis. Previous studies reported a benzimidazole series as potent cruzain inhibitors. Results & methodology: Considering the high similarity between these proteases, we evaluated 40 benzimidazoles against rhodesain. We describe their structure-activity relationships (SAR), revealing trends similar to those observed for cruzain and features that lead to enzyme selectivity. This series comprises noncovalent competitive inhibitors (best Ki = 0.21 μM against rhodesain) and micromolar activity against Trypanosoma brucei brucei. A cheminformatics analysis confirms scaffold novelty, and the inhibitors described have favorable predicted physicochemical properties. Conclusion: Our results support this series as a starting point for new human African trypanosomiasis medicines.

Recent Updates on Development of Drug Molecules for Human African Trypanosomiasis

2016 ◽  
Vol 16 (20) ◽  
pp. 2245-2265 ◽  
Author(s):  
Ajmer Singh Grewal ◽  
Deepti Pandita ◽  
Shashikant Bhardwaj ◽  
Viney Lather
Keyword(s):  
Human African Trypanosomiasis ◽  
African Trypanosomiasis ◽  
Drug Molecules

New Pd-Fe ferrocenyl antiparasitic compounds with bioactive 8-hydroxyquinoline ligands: a comparative study with their Pt-Fe analogues

2021 ◽  
Author(s):  
Feriannys Rivas ◽  
Andrea Medeiros ◽  
Cristina Quiroga ◽  
Diego Benítez ◽  
Marcelo Comini ◽  
...  
Keyword(s):  
Comparative Study ◽  
Trypanosoma Brucei ◽  
Human African Trypanosomiasis ◽  
African Trypanosomiasis

In the search for a more effective chemotherapy for the treatment of Human African Trypanosomiasis, the disease caused by the parasite Trypanosoma brucei, the development of ferrocenyl compounds has arisen...

Human African trypanosomiasis: Potential therapeutic benefits of an alternative suramin and melarsoprol regimen

2002 ◽  
Vol 51 (4) ◽  
pp. 381-388 ◽  
Author(s):  
Frank W Jennings ◽  
Jean Rodgers ◽  
Barbara Bradley ◽  
George Gettinby ◽  
Peter G.E Kennedy ◽  
...  
Keyword(s):  
Human African Trypanosomiasis ◽  
African Trypanosomiasis ◽  
Therapeutic Benefits

scholarly journals Human African trypanosomiasis in endemic focus of Abraka, Nigeria

2010 ◽  
Vol 3 (6) ◽  
pp. 448-450 ◽  
Author(s):  
Onyebiguwa Patrick Goddey Nmorsi ◽  
Clement Isaac ◽  
Igho Benjamin Igbinosa ◽  
Duncan Ogheneocovo Umukoro ◽  
Dafe Palmer Aitaikuru
Keyword(s):  
Human African Trypanosomiasis ◽  
African Trypanosomiasis ◽  
Endemic Focus
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