[HTML][HTML] Recent progress in the development of indole-based compounds active against malaria, trypanosomiasis and leishmaniasis

PAF Pacheco, MMM Santos - Molecules, 2022 - mdpi.com
Human protozoan diseases represent a serious health problem worldwide, affecting mainly
people in social and economic vulnerability. These diseases have attracted little investment …

Polyamine-trypanothione pathway: an update

A Ilari, A Fiorillo, I Genovese… - Future Medicinal Chemistry, 2017 - Taylor & Francis
In trypanosomatids, polyamine and trypanothione pathways can be considered as a whole
unique metabolism, where most enzymes are essential for parasitic survival and infectivity …

Drug-like molecules with anti-trypanothione synthetase activity identified by high throughput screening

D Benítez, J Franco, F Sardi, A Leyva… - Journal of enzyme …, 2022 - Taylor & Francis
Trypanothione synthetase (TryS) catalyses the synthesis of N 1, N8-bis (glutathionyl)
spermidine (trypanothione), which is the main low molecular mass thiol supporting several …

[HTML][HTML] The indole motif is essential for the antitrypanosomal activity of N5-substituted paullones

I Ihnatenko, MJ Müller, OCF Orban, JC Lindhof… - Plos one, 2023 - journals.plos.org
Severe infections with potentially fatal outcomes are caused by parasites from the genera
Trypanosoma and Leishmania (class Kinetoplastea). The diseases affect people of remote …

Direct C− H Arylation of Indole‐3‐Acetic Acid Derivatives Enabled by an Autonomous Self‐Optimizing Flow Reactor

N Vasudevan, E Wimmer, E Barré… - Advanced Synthesis …, 2021 - Wiley Online Library
Described herein is a continuous‐flow strategy for the palladium‐catalyzed direct C− H
arylation of indole‐3‐acetic acid derivatives with arenediazonium salts. A fully autonomous …

Recent advancement in the search of innovative antiprotozoal agents targeting trypanothione metabolism

F Saccoliti, R Di Santo, R Costi - ChemMedChem, 2020 - Wiley Online Library
Leishmania and Trypanosoma parasites are responsible for the challenging neglected
tropical diseases leishmaniases, Chagas disease, and human African trypanosomiasis …

The thiol-polyamine metabolism of Trypanosoma cruzi: molecular targets and drug repurposing strategies

A Talevi, C Carrillo, M Comini - Current Medicinal Chemistry, 2019 - ingentaconnect.com
Chagas´ disease continues to be a challenging and neglected public health problem in
many American countries. The etiologic agent, Trypanosoma cruzi, develops intracellularly …

Trypanothione synthetase confers growth, survival advantage and resistance to anti-protozoal drugs in Trypanosoma cruzi

AC Mesías, N Sasoni, DG Arias, CP Brandán… - Free Radical Biology …, 2019 - Elsevier
Background Chagas cardiomyopathy, caused by Trypanosoma cruzi infection, continues to
be a neglected illness, and has a major impact on global health. The parasite undergoes …

Computational approaches for drug discovery against trypanosomatid-caused diseases

CA Pereira, M Sayé, C Reigada, AM Silber… - Parasitology, 2020 - cambridge.org
During three decades, only about 20 new drugs have been developed for malaria,
tuberculosis and all neglected tropical diseases (NTDs). This critical situation was reached …

Mechanistic and biological characterisation of novel N5-substituted paullones targeting the biosynthesis of trypanothione in Leishmania

A Medeiros, D Benítez, RS Korn… - Journal of Enzyme …, 2020 - Taylor & Francis
Trypanothione synthetase (TryS) produces N 1, N8-bis (glutathionyl) spermidine (or
trypanothione) at the expense of ATP. Trypanothione is a metabolite unique and essential …