Results 1 to 10 of about 3,386 (154)

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   +7 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

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

In Silico Studies and Biological Evaluation of Thiosemicarbazones as Cruzain-Targeting Trypanocidal Agents for Chagas Disease [PDF]

Pharmaceutics
Background/Objectives: Chagas disease remains a major unmet medical need due to the limited efficacy and safety of current therapies. Here, we investigated sixteen thiosemicarbazone (TSC) derivatives as cruzain inhibitors using an integrated in silico/in
Lidiane Meier, Milena F. C. V. de Melo, Heitor R. Abreu, Isabella M. e Oliveira, Larissa Sens, Thiago H. Doring, Renata Krogh, Adilson Beatriz, Adriano D. Andricopulo, Sumbal Saba, Aldo S. de Oliveira, Jamal Rafique   +11 more
doaj   +5 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

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

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

Exploring 6-Hydroxy-3-Aryl/Heteroarylcoumarins as Promising Candidates Against Trypanosoma cruzi. [PDF]

ChemMedChem
New therapies are urgently needed for Chagas disease, and screening of 6‐hydroxy‐3‐aryl/heteroarylcoumarin derivatives identified highly selective compounds with potent activity against T. cruzi. In particular, derivative 1f showed submicromolar trypomastigote potency, dual‐stage activity, and inhibition of amastigote‐to‐trypomastigote differentiation,
Pereira CN, Lara LDS, Lanera SDC, Souza TP, Pereira MCS, Delogu GL, Santos MSD, Matos MJ.   +7 more
europepmc   +2 more sources

Repositioning FDA-Approved Sulfonamide-Based Drugs as Potential Carbonic Anhydrase Inhibitors in Trypanosoma cruzi: Virtual Screening and In Vitro Studies [PDF]

Pharmaceuticals
Background/Objectives: α-carbonic anhydrase (α-TcCA) has emerged as a promising drug target in T. cruzi, the causative agent of Chagas disease in the Americas. Sulfonamides, known inhibitors of CAs, bind to the zinc ion on the enzyme’s active site.
Eyra Ortiz-Pérez, Adriana Moreno-Rodríguez, Timoteo Delgado-Maldonado, Jessica L. Ortega-Balleza, Alonzo González-González, Alma D. Paz-González, Karina Vázquez, Guadalupe Avalos-Navarro, Simone Giovannuzzi, Claudiu T. Supuran, Gildardo Rivera   +10 more
doaj   +2 more sources