Results 11 to 20 of about 3,404 (180)

Evaluating 5-nitrofurans as trypanocidal agents. [PDF]

Antimicrob Agents Chemother, 2013
ABSTRACTThe nitroheterocycle nifurtimox, as part of a nifurtimox-eflornithine combination therapy, represents one of a limited number of treatments targetingTrypanosoma brucei, the causative agent of human African trypanosomiasis. The mode of action of this prodrug involves an initial activation reaction catalyzed by a type I nitroreductase (NTR), an ...
Bot C, Hall BS, Alvarez G, Di Maio R, González M, Cerecetto H, Wilkinson SR.   +6 more
europepmc   +6 more sources

Evaluating 5-Nitrothiazoles as Trypanocidal Agents. [PDF]

Antimicrob Agents Chemother, 2016
ABSTRACTThe growth-inhibitory properties of a 5-nitrothiazole series were evaluated againstTrypanosoma brucei. A subset of related compounds displayed the greatest potency toward the parasite while exhibiting little cytotoxic effect on mammalian cells, with this antiparasitic activity dependent on expression of a type I nitroreductase by the ...
O'Shea IP, Shahed M, Aguilera-Venegas B, Wilkinson SR.   +3 more
europepmc   +6 more sources

Evaluation of substituted ebselen derivatives as potential trypanocidal agents. [PDF]

Bioorg Med Chem Lett, 2017
Human African trypanosomiasis is a disease of sub-Saharan Africa, where millions are at risk for the illness. The disease, commonly referred to as African sleeping sickness, is caused by an infection by the eukaryotic pathogen, Trypanosoma brucei. Previously, a target-based high throughput screen revealed ebselen (EbSe), and its sulfur analog, EbS, to ...
Gordhan HM, Patrick SL, Swasy MI, Hackler AL, Anayee M, Golden JE, Morris JC, Whitehead DC.   +7 more
europepmc   +5 more sources

Quinol derivatives as potential trypanocidal agents.

Bioorg Med Chem, 2012
Quinols have been developed as a class of potential anti-cancer compounds. They are thought to act as double Michael acceptors, forming two covalent bonds to their target protein(s). Quinols have also been shown to have activity against the parasite Trypanosoma brucei, the causative organism of human African trypanosomiasis, but they demonstrated ...
Capes A, Patterson S, Wyllie S, Hallyburton I, Collie IT, McCarroll AJ, Stevens MF, Frearson JA, Wyatt PG, Fairlamb AH, Gilbert IH.   +10 more
europepmc   +5 more sources

New Lipophilic Hydroxamates as Promising Trypanocidal Agents: Design, Synthesis, SAR, and Conformational Behavior Studies. [PDF]

ACS Med Chem Lett
A series of novel hydroxamic acid derivatives was designed and synthesized, and their growth inhibitory activity against bloodstream form Trypanosoma brucei was evaluated. These compounds are based on conformationally constrained, lipophilic, spiro carbocyclic 2,6-diketopiperazine (2,6-DKP) scaffolds and bear a side pharmacophoric functionality that ...
Fytas G, Zoidis G, Drakopoulos A, Taylor MC, Kelly JM, Tsatsaroni A, Tsotinis A.   +6 more
europepmc   +5 more sources

Mechanistic Exploration of N,N′-Disubstituted Diamines as Promising Chagas Disease Treatments [PDF]

Pharmaceuticals
Introduction: Chagas disease, caused by the protozoan Trypanosoma cruzi, remains a major public health concern due to the limited effectiveness of current treatments, especially in the chronic stage.
Alejandro I. Recio-Balsells, Chantal Reigada, María Gabriela Mediavilla, Esteban Panozzo-Zénere, Miguel Villarreal Parra, Patricia S. Doyle, Juan C. Engel, Claudio A. Pereira, Julia A. Cricco, Guillermo R. Labadie   +9 more
doaj   +2 more sources

Benzopyrazine-Based Small Molecule Inhibitors As Trypanocidal and Leishmanicidal Agents: Green Synthesis, In Vitro, and In Silico Evaluations [PDF]

Frontiers in Chemistry, 2021
World Health Organization (WHO) identified twenty tropical disease categories as neglected tropical diseases (NTDs)1. Chagas’ disease (also known as American trypanosomiasis) and leishmaniasis are two major classes of NTDs. The total number of mortality,
Jonathan Rock, Daniel Garcia, Omar Espino, Shaila A. Shetu, Manuel J. Chan-Bacab, Rosa Moo-Puc, Navin B. Patel, Gildardo Rivera, Debasish Bandyopadhyay, Debasish Bandyopadhyay   +9 more
doaj   +2 more sources

Prevention of congenital chagas disease by trypanocide treatment in women of reproductive age: A meta-analysis of observational studies. [PDF]

PLoS Neglected Tropical Diseases
BackgroundMaternal-foetal transmission of Chagas disease (CD) affects newborns worldwide. Although Benznidazole and Nifurtimox therapies are the standard treatments, their use during pregnancy is contra-indicated.
Francisco Cezar Aquino de Moraes, Maria Eduarda Cavalcanti Souza, Lucca Dal Moro, Isabelle Batista Donadon, Emanuele Rocha da Silva, Dilma do Socorro Moraes de Souza, Rommel Mario Rodríguez Burbano   +6 more
doaj   +2 more sources

In Silico Investigation of TATA-Binding Protein as a Therapeutic Target for Chagas Disease: Insights into FDA Drug Repositioning [PDF]

Pharmaceuticals
Background: Parasitic diseases, particularly Chagas disease caused by Trypanosoma cruzi, primarily affect developing countries but are now spreading to wealthier nations due to changing migration patterns. With approximately 8 to 9 million cases annually
Carlos Gaona-López, Domingo Méndez-Álvarez, Alonzo Gonzalez-Gonzalez, Guadalupe Avalos-Navarro, Alma D. Paz-González, Adriana Moreno-Rodríguez, Benjamín Nogueda-Torres, Gildardo Rivera   +7 more
doaj   +2 more sources

Terpenoid Derivatives as Potential Trypanocidal Agents [PDF]

Medicinal chemistry, 2016
In this review we refer to a promising family of molecules in the fight against Chagas disease. Terpene derivatives are abundant in the plant Kingdom and in the last years many compounds have shown important biological activities. Diterpenes and sesquiterpene lactones have shown in vitro and in vivo trypanocidal activity and they emerge as potential ...
Esteban Lozano, Patricia Barrera
  +5 more sources