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Giardia duodenalis flavohemoglobin is a target of 5-nitroheterocycle and benzimidazole compounds acting as enzymatic inhibitors or subversive substrates.
Free Radic Biol Med
December 2024
Departamento de Genética y Biología Molecular, Centro de Investigación y de Estudios Avanzados Del Instituto Politécnico Nacional, 07360, Mexico City, Mexico. Electronic address:
Giardia duodenalis causes giardiasis in humans, companion, livestock and wild animals. Control of infection involves drugs as benzimidazoles (e.g.
View Article and Find Full Text PDFVaginal Tritrichomonas foetus infection in mice as an in vivo model for drug development against Trichomonas vaginalis.
PLoS One
October 2024
Department of Medicine, University of California San Diego, La Jolla, California, United States of America.
Article Synopsis
- Trichomonas vaginalis causes trichomoniasis, a widespread STD that affects over a hundred million people, and resistance to common treatments like metronidazole is increasing.
- The study explored using Tritrichomonas foetus, a related parasite, as a better animal model for testing new treatments since it caused reliable infections in mice, unlike T. vaginalis.
- Findings showed that while some drugs had similar effectiveness on both parasites, proteasome inhibitors were less effective on T. foetus, suggesting the need for targeted drug development and further understanding of genetic differences between the two organisms.
In vitro trypanocidal potency and in vivo treatment efficacy of oligomeric ethylene glycol-tethered nitrofurantoin derivatives.
Eur J Pharm Sci
January 2024
National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Inada, Obihiro, Hokkaido 080-8555, Japan.
African trypanosomiasis is a significant vector-borne disease of humans and animals in the tsetse fly belt of Africa, particularly affecting production animals such as cattle, and thus, hindering food security. Trypanosoma congolense (T. congolense), the causative agent of nagana, is livestock's most virulent trypanosome species.
View Article and Find Full Text PDFAntiprotozoal Activity of Benzoylthiourea Derivatives against : Insights into Mechanism of Action.
Pathogens
August 2023
Graduate Program in Microbiology, Department of Microbiology, State University of Londrina, Londrina 86057-970, Brazil.
For decades, only two nitroheterocyclic drugs have been used as therapeutic agents for Chagas disease. However, these drugs present limited effectiveness during the chronic phase, possess unfavorable pharmacokinetic properties, and induce severe adverse effects, resulting in low treatment adherence. A previous study reported that -(cyclohexylcarbamothioyl) benzamide (), -(-butylcarbamothioyl) benzamide (), and (4-bromo--(3-nitrophenyl) carbamothioyl benzamide () present selective antiprotozoal activity against all developmental forms of Y strain.
View Article and Find Full Text PDFEnzymatic Redox Properties and Cytotoxicity of Irreversible Nitroaromatic Thioredoxin Reductase Inhibitors in Mammalian Cells.
Int J Mol Sci
August 2023
Department of Xenobiotics Biochemistry, Institute of Biochemistry of Vilnius University, Sauletekio 7, LT-10257 Vilnius, Lithuania.
NADPH:thioredoxin reductase (TrxR) is considered a potential target for anticancer agents. Several nitroheterocyclic sulfones, such as Stattic and Tri-1, irreversibly inhibit TrxR, which presumably accounts for their antitumor activity. However, it is necessary to distinguish the roles of enzymatic redox cycling, an inherent property of nitroaromatics (ArNO), and the inhibition of TrxR in their cytotoxicity.
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