[HTML][HTML] Rate-of-Kill (RoK) assays to triage large compound sets for Chagas disease drug discovery: Application to GSK Chagas Box

J Cantizani, P Gamallo, I Cotillo… - … tropical diseases, 2021 - journals.plos.org
… Therefore, we propose that a drug discovery program should pursue an optimisation trajectory
towards compounds belonging to k-means cluster 2 falling on bottom-left quadrant I of the …

Targeting cysteine proteases in trypanosomatid disease drug discovery

LG Ferreira, AD Andricopulo - Pharmacology & therapeutics, 2017 - Elsevier
… design (SBDD), and medicinal chemistry efforts targeting cysteine proteases in Chagas
disease and HAT drug discovery will be discussed. Structural aspects of enzyme-inhibitor …

[HTML][HTML] Experimental and clinical treatment of Chagas disease: a review

PAS Junior, I Molina, SMF Murta… - The American journal …, 2017 - ncbi.nlm.nih.gov
Drug development for tropical diseases has largely relied on three strategies: label extension,
piggyback discovery, and de novo drug discovery. Label extension consists of extending …

[HTML][HTML] Introduction: drug discovery and development for neglected diseases

LS Goupil, JH McKerrow - Chemical Reviews, 2014 - ACS Publications
… As with other neglected diseases, the current drug therapy for Chagas Disease has many
drawbacks. Two drugs are routinely used, benznidazole and nifurtimox (Figure 3). As noted by …

[HTML][HTML] Advances in the treatment of Chagas disease: Promising new drugs, plants and targets

P García-Huertas, N Cardona-Castro - Biomedicine & Pharmacotherapy, 2021 - Elsevier
… explain why treatment so often fails to cure Chagas disease [14]. Thus, many efforts … Chagas
disease. Several experts in the drug discovery field and the Drugs for Neglected Diseases

Targets and patented drugs for chemotherapy of Chagas disease in the last 15 years-period

VG Duschak - Recent patents on anti-infective drug discovery, 2016 - ingentaconnect.com
… Top series of xanthine have been recently identified as clinical candidate for Chagas disease
Conclusion: In summary, loans on anti-Chagas disease agents focused to specific parasite …

[HTML][HTML] Utilizing Chemical Genomics to Identify Cytochrome b as a Novel Drug Target for Chagas Disease

S Khare, SL Roach, SW Barnes, D Hoepfner… - PLoS …, 2015 - journals.plos.org
… GNF7686 represents a promising starting point for Chagas disease drug discovery as it
potently inhibits growth of intracellular T. cruzi amastigotes with a half maximal effective …

[HTML][HTML] Aptamer-based detection of disease biomarkers in mouse models for chagas drug discovery

FF de Araujo, R Nagarkatti, C Gupta… - … Tropical Diseases, 2015 - journals.plos.org
… cruzi biomarker in blood and validate murine drug discovery models of Chagas disease. In
two … They suggest that the ELA assay can be used in drug discovery applications to assess …

Diversity-oriented synthesis yields a new drug lead for treatment of Chagas disease

S Dandapani, AR Germain, I Jewett… - ACS medicinal …, 2014 - ACS Publications
… treating the chronic phase of Chagas disease, ML341 is an attractive starting point for
developing drugs against both acute and chronic stages of Chagas disease. Results from further …

[HTML][HTML] Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

MC Field, D Horn, AH Fairlamb… - Nature Reviews …, 2017 - nature.com
… for drug discovery is to reposition drugs from other disease … need to refine the drug discovery
pathway for Chagas disease, in … made in drug discovery to find potential new drugs to treat …