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 …

NRF2 activation by nitrogen heterocycles: a review

MC Egbujor, P Tucci, UC Onyeije, CN Emeruwa… - Molecules, 2023 - mdpi.com
Several nitrogen heterocyclic analogues have been applied to clinical practice, and about
75% of drugs approved by the FDA contain at least a heterocyclic moiety. Thus, nitrogen …

Pd-catalyzed synthesis, characterization, and biological evaluations of pyrazole derivatives: DFT, molecular modelling and antioxidant studies

R Mehandi, C Twala, A Ali, S Ahmedi, M Rana… - Journal of …, 2024 - Elsevier
Abstract Using Pd (PPh 3) 4 as a catalyst, a new series of coupling products (5a–5l)
synthesized from pyrazole derivatives (4a-4c) and substituted boronic acids. Afterward, 1 H …

[HTML][HTML] Drug screening and development cascade for Chagas disease: an update of in vitro and in vivo experimental models

MNC Soeiro, PA Sales-Junior, VRA Pereira… - Memórias do Instituto …, 2024 - SciELO Brasil
Chagas disease is a tropical neglected disease that affects millions of people worldwide, still
demanding a more effective and safer therapy, especially in its chronic phase which lacks a …

New drug discovery strategies for the treatment of benznidazole-resistance in Trypanosoma cruzi, the causative agent of Chagas disease

SMF Murta, PA Lemos Santana… - Expert Opinion on …, 2024 - Taylor & Francis
Introduction Benznidazole, the drug of choice for treating Chagas Disease (CD), has
significant limitations, such as poor cure efficacy, mainly in the chronic phase of CD …

Bioactivity of Novel Pyrazole-Thiazolines Scaffolds against Trypanosoma cruzi: Computational Approaches and 3D Spheroid Model on Drug Discovery for Chagas …

LS Lara, GC Lechuga, LMR Orlando, BS Ferreira… - Pharmaceutics, 2022 - mdpi.com
Chagas disease, a century-old disease that mainly affects the impoverished population in
Latin America, causes high morbidity and mortality in endemic countries. The available …

Exo-or endo-1 H-pyrazole metal coordination modulated by the polyamine chain length in [1+ 1] condensation azamacrocycles. Binuclear complexes with remarkable …

I Bonastre-Sabater, A Lopera… - Dalton …, 2024 - pubs.rsc.org
The Cu2+ complexes of three [1+ 1] azacyclophane macrocycles having the 1H-pyrazole
ring as the spacer and the pentaamine 1, 5, 8, 11, 15-pentaazadecane (L1) or hexaamines …

[HTML][HTML] Synthesis and Anti-Trypanosoma cruzi Activity of New Pyrazole-Thiadiazole Scaffolds

TP Souza, LMR Orlando, LS Lara, VB Paes, LP Dutra… - Molecules, 2024 - mdpi.com
Chagas disease, a silent but widespread disease that mainly affects a socioeconomically
vulnerable population, lacks innovative safe drug therapy. The available drugs …

Antitrypanosomal Activity of 1, 2, 3-Triazole-Based Hybrids Evaluated Using In Vitro Preclinical Translational Models

LMR Orlando, LS Lara, GC Lechuga, GC Rodrigues… - Biology, 2023 - mdpi.com
Simple Summary Chagas disease, caused by the protozoan Trypanosoma cruzi, is a
neglected tropical disease that affects 6–7 million people worldwide. It is a global disease …

Engineered In Vitro Models to Improve the Mechanistic Understanding and Treatment of Neglected Tropical Diseases Caused by Protozoan Parasites

T Monjure, J Rosero, JA Ruley, AJ Hernandez… - GEN …, 2024 - liebertpub.com
Neglected tropical diseases (NTDs), particularly those caused by trypanosomatid protozoa,
impose a significant global burden, disproportionately affecting underserved communities in …