Results 1 to 10 of about 7,451 (168)

Novel African trypanocidal agents: membrane rigidifying peptides. [PDF]

PLoS ONE, 2012
The bloodstream developmental forms of pathogenic African trypanosomes are uniquely susceptible to killing by small hydrophobic peptides. Trypanocidal activity is conferred by peptide hydrophobicity and charge distribution and results from increased ...
John M Harrington, Chris Scelsi, Andreas Hartel, Nicola G Jones, Markus Engstler, Paul Capewell, Annette MacLeod, Stephen Hajduk   +7 more
doaj   +12 more sources

Evaluating 5-nitrofurans as trypanocidal agents. [PDF]

Antimicrob Agents Chemother, 2013
The nitroheterocycle nifurtimox, as part of a nifurtimox-eflornithine combination therapy, represents one of a limited number of treatments targeting Trypanosoma brucei, the causative agent of human African trypanosomiasis.
Bot C, Hall BS, Alvarez G, Di Maio R, González M, Cerecetto H, Wilkinson SR.   +6 more
europepmc   +7 more sources

Evaluating 5-Nitrothiazoles as Trypanocidal Agents. [PDF]

Antimicrob Agents Chemother, 2016
OA Monitor ExerciseOA Monitor ExerciseThe growth inhibitory properties of a 5-nitrothiazole series was evaluated against Trypanosoma brucei. A subset of related compounds displayed the greatest potency towards the parasite while exhibiting little ...
O'Shea IP, Shahed M, Aguilera-Venegas B, Wilkinson SR.   +3 more
europepmc   +7 more sources

TcSR62, an RNA-binding protein, as a new potential target for anti-trypanocidal agents [PDF]

Frontiers in Microbiology
Trypanosomatids are parasites of health importance that cause neglected diseases in humans and animals. Chagas’ disease, caused by Trypanosoma cruzi, affects 6–7 millions of people worldwide, mostly in Latin America, most of whom do not have access to ...
Analía G. Níttolo, Analía G. Níttolo, Agustina M. Chidichimo, Agustina M. Chidichimo, Ana L. Benacerraf, Timothy Cardozo, M. Clara Corso, M. Clara Corso, Valeria Tekiel, Valeria Tekiel, Javier G. De Gaudenzi, Javier G. De Gaudenzi, Gabriela Vanesa Levy, Gabriela Vanesa Levy   +13 more
doaj   +4 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   +4 more sources

In vitro genotoxicity of nitroimidazoles as a tool in the search of new trypanocidal agents [PDF]

Memorias do Instituto Oswaldo Cruz, 2019
BACKGROUND Only benznidazole (Bnz) (1) and nifurtimox (Nfx) (2) are licensed for the treatment of Chagas disease although their safety and efficacy profile are far from ideal. Farmanguinhos from Fiocruz has developed seven nitroimidazole compounds (4-10)
Ana Claudia Manoel Von Trompowsky, Taline Ramos Conde, Renata Calil Lemos, Bruna Maria CS Quaresma, Marcelly Cristina SR Pitombeira, Alcione Silva de Carvalho, Núbia Boechat, Kelly Salomão, Solange Lisboa de Castro, Helena Pereira da Silva Zamith   +9 more
doaj   +2 more sources

Synthesis of 1,2,6-Thiadiazin 1,1-Dioxide Derivatives as Trypanocidal Agents [PDF]

Molecules, 2000
It describes the synthesis of new 1,2,6-Thiadiazin 1,1-dioxide derivatives using condensation of the Knoevenagel type. The products are evaluated in vitro as trypanocidal agents.
H. Cerecetto, R. Di Maio, G. Seoane, C. Ochoa, S. Muelas, A. Gómez-Barrio   +5 more
doaj   +2 more sources

Molecular Docking-Based Virtual Screening of FDA-Approved Drugs Using Trypanothione Reductase Identified New Trypanocidal Agents [PDF]

Molecules
American trypanosomiasis or Chagas disease, caused by Trypanosoma cruzi (T. cruzi), affects approximately 6–7 million people worldwide. However, its pharmacological treatment causes several uncomfortable side effects, causing patients’ treatment ...
Rogelio Gómez-Escobedo, Domingo Méndez-Álvarez, Citlali Vázquez, Emma Saavedra, Karina Vázquez, Verónica Alcántara-Farfán, Joaquín Cordero-Martínez, Alonzo Gonzalez-Gonzalez, Gildardo Rivera, Benjamín Nogueda-Torres   +9 more
doaj   +2 more sources

Mapping the S1 and S1' subsites of cysteine proteases with new dipeptidyl nitrile inhibitors as trypanocidal agents. [PDF]

PLoS Neglected Tropical Diseases, 2020
The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. A series of 26 new compounds were designed, synthesized, and tested against the recombinant cruzain (Cz) to map its S1/
Lorenzo Cianni, Carina Lemke, Erik Gilberg, Christian Feldmann, Fabiana Rosini, Fernanda Dos Reis Rocho, Jean F R Ribeiro, Daiane Y Tezuka, Carla D Lopes, Sérgio de Albuquerque, Jürgen Bajorath, Stefan Laufer, Andrei Leitão, Michael Gütschow, Carlos A Montanari   +14 more
doaj   +2 more sources

Identification of Novel Trypanosoma cruzi Cysteine Protease Inhibitors via Ligand-Based Virtual Screening of FDA-Approved Drugs with Trypanocidal Activity [PDF]

Diseases
Background: Chagas disease is a major public health problem, especially in Latin American countries, and benznidazole and nifurtimox are currently the only drugs available for its treatment.
Lenci K. Vázquez-Jiménez, Alonzo González-González, Timoteo Delgado-Maldonado, Rogelio Gómez-Escobedo, Benjamín Nogueda-Torres, Ana Verónica Martínez-Vázquez, Eyrá Ortiz-Pérez, Charmina Aguirre-Alvarado, Verónica Alcántara-Farfán, Joaquín Cordero-Martínez, Lorena Rodríguez-Páez, Adriana Moreno-Rodriguez, Gildardo Rivera   +12 more
doaj   +2 more sources