A5033685924- Trypanosoma species research and implications
- Research on Leishmaniasis Studies
- Synthesis and Biological Evaluation
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Biochemical and Molecular Research
- HIV Research and Treatment
- Comparative Literary Analysis and Criticism
- Spanish Literature and Culture Studies
- Cultural and Mythological Studies
- Bioactive Compounds and Antitumor Agents
- Synthesis and biological activity
- Parasites and Host Interactions
- Early Modern Spanish Literature
- Microbial Natural Products and Biosynthesis
- Toxin Mechanisms and Immunotoxins
- Libraries, Manuscripts, and Books
- Helminth infection and control
- HIV/AIDS drug development and treatment
- Insect Pest Control Strategies
- Business, Education, Mathematics Research
- Protein Structure and Dynamics
- Archaeological and Historical Studies
- Bacteriophages and microbial interactions
- Latin American history and culture
Universidad de la República
2016-2025
Instituto de Biologia Experimental e Tecnológica
2017
Rede de Química e Tecnologia
2017
Instituto de Química Orgánica General
2017
Universidad La República
2017
Instituto Politécnico Nacional
2016
Tecnológico Nacional de México
2016
Universidad Autónoma de Madrid
2001
The neglected illness Chagas disease is treated with limited efficacy and adverse effects by old drugs. Due to the low interest of pharmaceutical industry in targeting economically depressed-patients, repurposing a tool that should be applied because it can introduce new anti-Chagas entities into clinic at reduced costs. To investigate repurposing/combination medicines strategies as treatment. Epimastigotes, trypomastigotes amastigotes Trypanosoma cruzi were vitro exposed 28...
Chagas disease, caused by Trypanosoma cruzi parasite, was described thousands of years ago. Currently, it affects millions people, mostly in Latin America, and there are not suitable drugs for treating it. As an attempt to find appropriate deal with this problem, we report here on the design, synthesis, characterization 82 new compounds. Trypanosomicidal behavior vitro showed more than 20 outstanding derivatives anti-Trypanosoma activity. Furthermore, studied nonspecific toxicity against...
ABSTRACT Although the parasitic infection Chagas' disease was described over 100 years ago, even now there are not suitable drugs. The available drugs nifurtimox and benznidazole have limited efficacies tolerances, with proven mutagenic effects. Attempting to find appropriate deal this problem, here we report on development pharmacological characterization of new amide-containing thiazoles. In present study, evaluated in vitro vivo effects candidates against Trypanosoma cruzi , etiological...
Nematode parasites have a profound impact on humankind, infecting nearly one-quarter of the world's population, as well livestock. There is pressing need for discovering nematicides due to spread resistance currently used drugs. The free-living nematode Caenorhabditis elegans formidable experimentally tractable model organism that offers key advantages in accelerating nematicide discovery. We report screening drug-like libraries using an overnight high-throughput C. assay, based automated...
Abstract Triosephosphate isomerase (TIM) is an essential Trypanosoma cruzi enzyme and one of the few validated drug targets for Chagas disease. The known inhibitors this behave poorly or have low activity in parasite. In work, we used symmetrical diarylideneketones derived from structures with trypanosomicidal activity. We obtained enzymatic inhibitor IC 50 value 86 n m without inhibition effects on mammalian enzyme. These molecules also affected cruzipain, another proteolytic This dual...
ABSTRACT The nitroheterocycle nifurtimox, as part of a nifurtimox-eflornithine combination therapy, represents one limited number treatments targeting Trypanosoma brucei , the causative agent human African trypanosomiasis. mode action this prodrug involves an initial activation reaction catalyzed by type I nitroreductase (NTR), enzyme found predominantly in prokaryotes, leading to formation cytotoxic unsaturated open-chain nitrile metabolite. Here, we evaluate trypanocidal activities library...
Favipiravir is an important selective antiviral against RNA-based viruses, and currently, it being repurposed as a potential drug for the treatment of COVID-19. This type chemical system presents different carboxamide-rotameric hydroxyl-tautomeric states, which could be essential interpreting its activity. Herein, tautomeric 3-hydroxypyrazine/3-pyrazinone pair favipiravir 6-substituted analogues, 6-Cl, 6-Br, 6-I, 6-H, were fully investigated in solution solid state through...
A series of fifty arylideneketones and thiazolidenehydrazines was evaluated against Leishmania infantum braziliensis. Furthermore, new simplified thiazolidenehydrazine derivatives were Trypanosoma cruzi. The cytotoxicity the active compounds on non-infected fibroblasts or macrophages established in vitro to evaluate selectivity their anti-parasitic effects. Seven ten had good activity three parasites. IC50 values for T. cruzi spp. ranged from 90 nM-25 µM. Eight multi-trypanocidal (the...
Prostate cancer is the most common in men around world. It a complex and heterogeneous disease which androgens their receptors play crucial role progression development. The current treatment for prostate combination of surgery, hormone therapy, radiation chemotherapy. Therapeutic agents commonly used clinic include steroidal non-steroidal anti-androgens, such as cyproterone acetate, bicalutamide enzalutamide. These few have multiple adverse effects are not 100% effective. Several plant...
Stevia species (Asteraceae) have been a rich source of terpenoid compounds, mainly sesquiterpene lactones, several which show antiprotozoal activity. In the search for new trypanocidal S. satureiifolia var. and alpina were studied. Two santhemoidin C 2-oxo-8-deoxyligustrin, respectively, isolated. These compounds assessed in vitro against Trypanosoma cruzi stages, showing IC50 values 11.80 4.98 on epimastigotes, 56.08 26.19 trypomastigotes 4.88 20.20 µM amastigotes, respectively....
A novel efficient one-step synthetic strategy for the preparation of antiviral favipiravir from with available 3-hydroxy-2-pyrazinecarboxamide and Selectfluor® was developed, use an IL being essential.
Introduction: The identification of chemical compounds that interfere with SARS-CoV-2 replication continues to be a priority in several academic and pharmaceutical laboratories. Computational tools approaches have the power integrate, process analyze multiple data short time. However, these initiatives may yield unrealistic results if applied models are not inferred from reliable resulting predictions confirmed by experimental evidence. Methods: We undertook drug discovery campaign against...
Context: Triosephosphate isomerase (TIM) is a ubiquitous enzyme that has been targeted for the discovery of new small molecular weight compounds used against Trypanosoma cruzi, causative agent Chagas disease. We have identified phenazine and 1,2,6-thiadiazine chemotypes as novel inhibitors TIM from T. cruzi (TcTIM).Objective: Study mechanism TcTIM inhibition by derivative derivative.Methods: performed biochemical theoretical docking studies to characterize interaction derivatives with...
The cattle tick Rhipicephalus microplus is one of the most important ectoparasites causing significant economic losses for industry. major tool control reducing number ticks, applying acaricides in cattle. However, overuse has led to selection resistant populations R. these products, some even more than active principle. Thus, exploration new molecules with acaricidal activity become necessary. Triosephosphate isomerase (TIM) an essential enzyme metabolism and could be interesting target...
Trematode infections such as schistosomiasis and fascioliasis cause significant morbidity in an estimated 250 million people worldwide the associated agricultural losses are at more than US$ 6 billion per year. Current chemotherapy is limited. Triosephosphate isomerase (TIM), enzyme of glycolytic pathway, has emerged a useful drug target many parasites, including Fasciola hepatica TIM (FhTIM). We identified 21 novel compounds that selectively inhibit this enzyme. Using microscale...
background To determine the efficacy and acceptability of deltamethrin‐impregnated bednets in controlling Chagas disease South America. methods In three endemic departments Colombia, a qualitative study on people's knowledge about disease, vectors, preventive measures their willingness for collaboration control oper‐ ations was undertaken. Additionally, an entomological with 100 laboratory‐bred vectors ( Rhodnius prolixus ), were released 5 nights (20 each night) experimental room, human...
Context: Triosephosphate isomerase (TIM) is a ubiquitous enzyme that has been targeted for the discovery of small molecular weight compounds with potential use against Trypanosoma cruzi, causative agent Chagas disease. We have identified new selective inhibitor chemotype TIM from T. cruzi (TcTIM), 1,2,4-thiadiazol-5(4H)-one.Objective: Study mechanism TcTIM inhibition by 1,2,4-thiadiazol derivative.Methods: performed biochemical characterization interaction derivative wild-type and mutant...
The current chemotherapy for Chagas disease is based on monopharmacology with low efficacy and drug tolerance. Polypharmacology one of the strategies to overcome these limitations.Study anti-Trypanosoma cruzi activity associations benznidazole (Bnz) three new synthetic T. cruzi-triosephosphate isomerase inhibitors, 2, 3, 4, in order potentiate their actions.The vitro effect combinations were determined constructing corresponding isobolograms. In vivo activities assessed using an acute murine...