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Cationic and anionic PLGA-cholesterol hybrid nanoparticles as promising platforms to enhance the trypanocidal efficacy of benznidazole and drug delivery in Trypanosoma cruzi-infected cells.
Biomed Pharmacother
January 2025
Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte-UFRN, Natal, RN, Brazil. Electronic address:
Chagas disease is a neglected tropical disease caused by the protozoan Trypanosoma cruzi, remains a significant global health challenge. Currently, benznidazole (BNZ) is the primary treatment in many countries. However, this drug is limited by low bioavailability, significant host toxicity, and reduced efficacy in chronic disease phase.
View Article and Find Full Text PDFIn vitro assays identified thiohydantoins with anti-trypanosomatid activity and molecular modelling studies indicated possible selective CYP51 inhibition.
Sci Rep
January 2025
Departamento de Química, Centro de Ciências Exatas, Universidade Estadual de Londrina, Londrina, PR, Brasil.
This work investigates the anti-trypanosomal activities of ten thiohydantoin derivatives against the parasite Trypanosoma cruzi. Compounds with aliphatic chains (THD1, THD3, and THD5) exhibited the most promising IC against the epimastigote form of T. cruzi.
View Article and Find Full Text PDFNew series of 3-pyridyl-1,3-thiazoles: In vitro and in vivo anti-Trypanosomatidae profile, in vitro and in silico mechanism of action approach.
Eur J Med Chem
December 2024
Laboratory of Planning in Medicinal Chemistry, Department of Pharmaceutical Sciences, Center for Health Sciences, Federal University of Pernambuco, 50740-535, Recife, PE, Brazil. Electronic address:
Trypanosomatidae diseases, such as Chagas disease and leishmaniasis, are caused by protozoan parasites of the Trypanosomatidae family, namely Trypanosoma cruzi and Leishmania species, respectively. There is an urgent need for new therapies. Both pyridine and thiazole rings are recognized as important scaffolds in medicinal chemistry.
View Article and Find Full Text PDFSynthesis strategies and anti-parasitic evaluation of novel compounds for chagas disease: Advancing drug discovery through structure-activity relationships.
Eur J Med Chem
December 2024
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, 144411, India. Electronic address:
This study presents a comprehensive exploration of the synthesis of novel compounds targeting Chagas Disease (CD) caused by Trypanosoma cruzi. It is a global health threat with over 6-7 million infections worldwide. Addressing challenges in current treatments, the investigation explores diverse compound classes, including thiazoles, thiazolidinone, imidazole, pyrazole, 1,6-diphenyl-1H-pyrazolo[3,4-b] pyridine, pyrrole, naphthoquinone, neolignan, benzeneacyl hydrazones, and chalcones-based compounds.
View Article and Find Full Text PDFGenome report: First whole genome sequence of Triatoma sanguisuga (Le Conte, 1855), vector of Chagas disease.
G3 (Bethesda)
December 2024
Department of Entomology and Wildlife Ecology, University of Delaware, Newark, DE 19716, USA.
Article Synopsis
- Triatoma sanguisuga, the most common triatomine bug in the US, carries the parasite Trypanosoma cruzi, responsible for Chagas disease, although diagnoses are rare in the country.
- The study presented the first complete genome sequence of T. sanguisuga, obtained from a specimen in Delaware, revealing a genome size of 1.162 Gbp with high assembly quality, evidenced by a 99.1% BUSCO score.
- This genomic information can enhance understanding of triatomine bugs in colder climates and support public health initiatives for managing vector-borne diseases.
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