[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 …

Designing drugs when there is low data availability: one-shot learning and other approaches to face the issues of a long-term concern

GC Verissimo, MSM Serafim… - Expert Opinion on …, 2022 - Taylor & Francis
Introduction Modern drug discovery is generally accessed by useful information from
previous large databases or uncovering novel data. The lack of biological and/or chemical …

Structure-Based Optimization of Quinazolines as Cruzain and TbrCATL Inhibitors

E Barbosa da Silva, DA Rocha, IS Fortes… - Journal of Medicinal …, 2021 - ACS Publications
The cysteine proteases, cruzain and Tbr CATL (rhodesain), are therapeutic targets for
Chagas disease and Human African Trypanosomiasis, respectively. Among the known …

The gene repertoire of the main cysteine protease of Trypanosoma cruzi, cruzipain, reveals four sub-types with distinct active sites

VC Santos, AER Oliveira, ACB Campos… - Scientific Reports, 2021 - nature.com
Cruzipains are the main papain-like cysteine proteases of Trypanosoma cruzi, the protozoan
parasite that causes Chagas disease. Encoded by a multigenic family, previous studies …

Molecular targets for Chagas disease: Validation, challenges and lead compounds for widely exploited targets

M Laureano de Souza, TJWJD Lapierre… - Expert Opinion on …, 2023 - Taylor & Francis
Introduction Chagas disease (CD) imposes social and economic burdens, yet the available
treatments have limited efficacy in the disease's chronic phase and cause serious adverse …

A comprehensive review on potential candidates for the treatment of chagas disease

S Pathak, M Bhardwaj, N Agrawal… - Chemical biology & …, 2023 - Wiley Online Library
Twenty different infectious disorders induced by bacteria, viruses, and parasites are
categorized as neglected tropical diseases (NTDs) by WHO. The severity of chagas disease …

Chloride substitution on 2-hydroxy-3, 4, 6-trimethoxyphenylchalcones improves in vitro selectivity on Trypanosoma cruzi strain Y

EP Magalhães, NDB Gomes, TA De Freitas… - Chemico-biological …, 2022 - Elsevier
Chagas disease is a disease that is emerging in North America and Europe countries.
Benznidazole is the main drug available, but it has high toxicity and low efficacy in the …

Experimental and computational study of aryl-thiosemicarbazones inhibiting cruzain reveals reversible inhibition and a stepwise mechanism

LC Martins, RB de Oliveira, J Lameira… - Journal of Chemical …, 2023 - ACS Publications
Trypanosoma cruzi is a parasite that infects about 6–7 million people worldwide, mostly in
Latin America, causing Chagas disease. Cruzain, the main cysteine protease of T. cruzi, is a …

Synthesis, Design, and Structure‐Activity Relationship of a Benzenesulfonylpiperazine Series against Trypanosoma cruzi

AC Cassiano Martinho, D de Melo Resende… - …, 2022 - Wiley Online Library
Chagas disease is a neglected tropical disease, endemic in Latin America and caused by
the protozoan parasite Trypanosoma cruzi. Available treatments show low cure efficacy …

Chagas disease drug discovery in Latin America—A mini review of antiparasitic agents explored between 2010 and 2021

RG de Oliveira, LR Cruz, MC Mollo, LC Dias… - Frontiers in …, 2021 - frontiersin.org
Chagas disease is a neglected tropical disease caused by the protozoan parasite
Trypanosoma cruzi that endangers almost 70 million people worldwide. The only two drugs …