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 +7 more
doaj +8 more sources
TcSR62, an RNA-binding protein, as a new potential target for anti-trypanocidal agents [PDF]
Frontiers in MicrobiologyTrypanosomatids 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 +13 more
doaj +6 more sources
Molecular Docking-Based Virtual Screening of FDA-Approved Drugs Using Trypanothione Reductase Identified New Trypanocidal Agents [PDF]
MoleculesAmerican 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 +9 more
doaj +4 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 +5 more
doaj +4 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 +14 more
doaj +4 more sources
Synthesis of New Hybrid Derivatives from Metronidazole and Eugenol Analogues as Trypanocidal Agents
Journal of Pharmacy & Pharmaceutical Sciences, 2021 Background: The search for new drug compounds is always challenging and there are several different strategies that involve the most varied and creative approaches in medicinal chemistry. One of them is the technique of molecular hybridisation: forming a
Mônica Fraccarolli Pelozo +8 more
doaj +5 more sources
In Silico Studies and Biological Evaluation of Thiosemicarbazones as Cruzain-Targeting Trypanocidal Agents for Chagas Disease [PDF]
PharmaceuticsBackground/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 +11 more
doaj +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 +9 more
doaj +4 more sources
Synthesis of 4-(4-chlorophenyl)thiazole compounds: in silico and in vitro evaluations as leishmanicidal and trypanocidal agents [PDF]
Anais da Academia Brasileira de Ciências, 2023 Neglected tropical diseases are a diverse group of communicable pathologies that mainly prevail in tropical and subtropical regions. Thus, the objective of this work was to evaluate the biological potential of eight 4-(4-chlorophenyl)thiazole compounds ...
IRANILDO JOSÉ DA CRUZ FILHO +4 more
doaj +3 more sources
Repositioning FDA-Approved Sulfonamide-Based Drugs as Potential Carbonic Anhydrase Inhibitors in Trypanosoma cruzi: Virtual Screening and In Vitro Studies [PDF]
PharmaceuticalsBackground/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 +10 more
doaj +2 more sources