State-of-the-art in the drug discovery pathway for Chagas disease: A framework for drug development and target validation

JC Gabaldón-Figueira… - … and Reports in …, 2023 - Taylor & Francis
Chagas disease is the most important protozoan infection in the Americas, and constitutes a
significant public health concern throughout the world. Development of new medications …

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 …

Cyanotriazoles are selective topoisomerase II poisons that rapidly cure trypanosome infections

SPS Rao, MK Gould, J Noeske, M Saldivia, RS Jumani… - Science, 2023 - science.org
Millions who live in Latin America and sub-Saharan Africa are at risk of trypanosomatid
infections, which cause Chagas disease and human African trypanosomiasis (HAT) …

Frequency variation and dose modification of benznidazole administration for the treatment of Trypanosoma cruzi infection in mice, dogs, and nonhuman primates

JM Bustamante, BE White, GK Wilkerson… - Antimicrobial agents …, 2023 - Am Soc Microbiol
Trypanosoma cruzi naturally infects a broad range of mammalian species and frequently
results in the pathology that has been most extensively characterized in human Chagas …

Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors

MG Thomas, K McGonagle, P Rowland… - Journal of Medicinal …, 2023 - ACS Publications
There is an urgent need for new treatments for Chagas disease, a parasitic infection which
mostly impacts South and Central America. We previously reported on the discovery of …

The landscape of small-molecule prodrugs

Z Fralish, A Chen, S Khan, P Zhou… - Nature Reviews Drug …, 2024 - nature.com
Prodrugs are derivatives with superior properties compared with the parent active
pharmaceutical ingredient (API), which undergo biotransformation after administration to …

Therapeutic Potential of Marine-Derived Cyclic Peptides as Antiparasitic Agents

R Ribeiro, L Costa, E Pinto, E Sousa, C Fernandes - Marine Drugs, 2023 - mdpi.com
Parasitic diseases still compromise human health. Some of the currently available
therapeutic drugs have limitations considering their adverse effects, questionable efficacy …

Immunopathogenesis in Trypanosoma cruzi infection: a role for suppressed macrophages and apoptotic cells

NS Vellozo, TC Matos-Silva, MF Lopes - Frontiers in Immunology, 2023 - frontiersin.org
During Trypanosoma cruzi infection, macrophages phagocytose parasites and remove
apoptotic cells through efferocytosis. While macrophage 1 (M1) produces proinflammatory …

Elemental exchange: Bioisosteric replacement of phosphorus by boron in drug design

NV Mehta, A Abhyankar, MS Degani - European Journal of Medicinal …, 2023 - Elsevier
Continuous efforts are being directed toward the employment of boron in drug design due to
its advantages and unique characteristics including a plethora of target engagement modes …

Further investigations of nitroheterocyclic compounds as potential antikinetoplastid drug candidates

C García-Estrada, Y Pérez-Pertejo… - Biomolecules, 2023 - mdpi.com
Due to the lack of specific vaccines, management of the trypanosomatid-caused neglected
tropical diseases (sleeping sickness, Chagas disease and leishmaniasis) relies exclusively …