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 …

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 …

From rational design to serendipity: discovery of novel thiosemicarbazones as potent trypanocidal compounds

SFP Braga, VC Santos, RP Vieira, EB da Silva… - European Journal of …, 2022 - Elsevier
Chagas disease is a major public health problem caused by Trypanosoma cruzi, with an
estimated 6–7 million people infected and 70 million at risk of infection. T. brucei gambiense …

Screening the Pathogen Box to Discover and Characterize New Cruzain and TbrCatL Inhibitors

T do Valle Moreira, LC Martins, LA Diniz… - Pathogens, 2023 - mdpi.com
Chagas disease and Human African Trypanosomiasis, caused by Trypanosoma cruzi and T.
brucei, respectively, pose relevant health challenges throughout the world, placing 65 to 70 …

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 …

Structure‐Activity Relationships, Tolerability and Efficacy of Microtubule‐Active 1,2,4‐Triazolo[1,5‐a]pyrimidines as Potential Candidates to Treat Human African …

L Monti, LJ Liu, C Varricchio, B Lucero, T Alle… - …, 2023 - Wiley Online Library
Tubulin and microtubules (MTs) are potential protein targets to treat parasitic infections and
our previous studies have shown that the triazolopyrimidine (TPD) class of MT‐active …

The Kavaratamides: Discovery of Linear Lipodepsipeptides from the Marine Cyanobacterium Moorena bouillonii Using a Comparative Chemogeographic Analysis

B Ryu, E Glukhov, TR Teixeira, CR Caffrey… - Journal of Natural …, 2024 - ACS Publications
Kavaratamide A (1), a new linear lipodepsipeptide possessing an unusual isopropyl-O-
methylpyrrolinone moiety, was discovered from the tropical marine filamentous …

Gallic acid alkyl esters: Trypanocidal and Leishmanicidal activity, and target identification via modeling studies

D Steverding, LG do Nascimento, Y Perez-Castillo… - Molecules, 2022 - mdpi.com
Eight gallic acid alkyl esters (1–8) were synthesized via Fischer esterification and evaluated
for their trypanocidal and leishmanicidal activity using bloodstream forms of Trypanosoma …

[HTML][HTML] Development of subunit selective proteasome substrates for Schistosoma species

Z Jiang, EB Silva, C Liu, P Fajtová, LJ Liu, N El-Sakkary… - bioRxiv, 2024 - ncbi.nlm.nih.gov
Schistosomiasis, or bilharzia, is a neglected tropical disease caused by Schistosoma spp.
blood flukes that infects over 200 million people worldwide. Just one partially effective drug …