[HTML][HTML] Examination of multiple Trypanosoma cruzi targets in a new drug discovery approach for Chagas disease

I Beltran-Hortelano, V Alcolea, M Font… - Bioorganic & medicinal …, 2022 - Elsevier
Chagas disease (CD) is a centenarian neglected parasitosis caused by the protozoan
Trypanosoma cruzi (T. cruzi). Despite the continuous efforts of many organizations and …

Technologies for Direct Detection of Covalent Protein–Drug Adducts

E Mons, RQ Kim, MPC Mulder - Pharmaceuticals, 2023 - mdpi.com
In the past two decades, drug candidates with a covalent binding mode have gained the
interest of medicinal chemists, as several covalent anticancer drugs have successfully …

Computer-aided design of 1, 4-naphthoquinone-based inhibitors targeting cruzain and rhodesain cysteine proteases

LR Silva, AS Guimaraes, J do Nascimento… - Bioorganic & Medicinal …, 2021 - Elsevier
Abstract Chagas disease and Human African Trypanosomiasis (HAT) are caused by
Trypanosoma cruzi and T. brucei parasites, respectively. Cruzain (CRZ) and Rhodesain …

Intramolecular Interactions Enhance the Potency of Gallinamide A Analogues against Trypanosoma cruzi

E Barbosa Da Silva, V Sharma… - Journal of Medicinal …, 2022 - ACS Publications
Gallinamide A, a metabolite of the marine cyanobacterium Schizothrix sp., selectively
inhibits cathepsin L-like cysteine proteases. We evaluated the potency of gallinamide A and …

Synthesis and Biological Evaluation of New Chalcogen Semicarbazone (S, Se) and Their Azole Derivatives against Chagas Disease

M Rubio-Hernández, V Alcolea… - Journal of Medicinal …, 2024 - ACS Publications
Chagas disease is caused by the eukaryote parasite Trypanosoma cruzi. Current treatment
exhibits limited efficacy and selenium-based compounds emerged as promising candidates …

Coumarin-based derivatives targeting Trypanosoma cruzi cruzain and Trypanosoma brucei cathepsin L-like proteases

JA Nunes, FN da Silva, EB da Silva… - New Journal of …, 2023 - pubs.rsc.org
The protozoa, Trypanosoma cruzi (etiological agent of Chagas diseases–also named
American trypanosomiasis) and T. brucei (causative agent of human African …

Antiparasitic Activity of Oxindolimine–Metal Complexes against Chagas Disease

MC Portes, GA Ribeiro, GL Sabino, RAA De Couto… - Inorganics, 2023 - mdpi.com
Some copper (II) and zinc (II) complexes with oxindolimine ligands were tested regarding
their trypanocidal properties. These complexes have already shown good biological activity …

Nanomolar activity of coumarin-3-thiosemicarbazones targeting Trypanosoma cruzi cruzain and the T. brucei cathepsin L-like protease

JA Nunes, PF da Silva Santos-Júnior… - European Journal of …, 2025 - Elsevier
Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei (T. brucei) urgently demand
innovative drug development due to their impact on public health worldwide. Their cysteine …

Identification of inhibitors as drug candidates against Chagas disease

SC Araujo, RM de Angelo, H Barbosa… - European Journal of …, 2023 - Elsevier
Chagas disease, after more than a century after its discovery, is still a major public health
problem. It is estimated that approximately 10 million people worldwide are infected with T …

Combining charge density analysis with machine learning tools to investigate the cruzain inhibition mechanism

AM Luchi, RN Villafañe, JL Gomez Chavez… - ACS …, 2019 - ACS Publications
Trypanosoma cruzi, a flagellate protozoan parasite, is responsible for Chagas disease. The
parasite major cysteine protease, cruzain (Cz), plays a vital role at every stage of its life cycle …