Results 1 to 10 of about 3,959 (186)

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   +8 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   +8 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   +6 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   +3 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   +5 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   +3 more sources

Natural and Semisynthetic Analogues of Manadoperoxide B Reveal New Structural Requirements for Trypanocidal Activity [PDF]

Marine Drugs, 2013
Chemical analysis of the Indonesian sponge Plakortis cfr. lita afforded two new analogues of the potent trypanocidal agent manadoperoxide B (1), namely 12-isomanadoperoxide B (2) and manadoperoxidic acid B (3).
Orazio Taglialatela-Scafati, Deniz Tasdemir, Marcel Kaiser, Henny A. Dien, Barbara Calcinai, Carlo Cerrano, Fernando Scala, Giuseppina Chianese   +7 more
doaj   +2 more sources

Ligand-Based Virtual Screening and Molecular Docking of Benzimidazoles as Potential Inhibitors of Triosephosphate Isomerase Identified New Trypanocidal Agents. [PDF]

Int J Mol Sci, 2022
Trypanosoma cruzi (T. cruzi) is a parasite that affects humans and other mammals. T. cruzi depends on glycolysis as a source of adenosine triphosphate (ATP) supply, and triosephosphate isomerase (TIM) plays a key role in this metabolic pathway.
Vázquez-Jiménez LK, Juárez-Saldivar A, Gómez-Escobedo R, Delgado-Maldonado T, Méndez-Álvarez D, Palos I, Bandyopadhyay D, Gaona-Lopez C, Ortiz-Pérez E, Nogueda-Torres B, Ramírez-Moreno E, Rivera G.   +11 more
europepmc   +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

An In Silico and In Vitro Approach Identified Potential Trypanothione Synthetase Inhibitors with Trypanocidal Activity [PDF]

Molecules
In this study, a drug repurposing strategy was implemented with the aim of identifying new trypanocidal agents against Trypanosoma cruzi (T. cruzi). A total of 924 Food and Drug Administration (FDA)-approved drugs were screened by molecular docking on ...
Rogelio Gómez-Escobedo, Domingo Méndez-Álvarez, Alma D. Paz-González, Eyra Ortiz-Pérez, Lenci K. Vázquez-Jiménez, Ana Verónica Martínez-Vázquez, Timoteo Delgado-Maldonado, José M. Quintero-Solano, Citlali Vázquez, Emma Saavedra, Guadalupe Avalos-Navarro, Karina Vázquez, Gildardo Rivera, Benjamín Nogueda-Torres   +13 more
doaj   +2 more sources