A5066886558- Helminth infection and control
- Parasites and Host Interactions
- Parasite Biology and Host Interactions
- Coccidia and coccidiosis research
- Crystallization and Solubility Studies
- Synthesis and biological activity
- Seaweed-derived Bioactive Compounds
- Pharmacological Effects and Toxicity Studies
- Drug Solubulity and Delivery Systems
- Nematode management and characterization studies
- Synthesis and Characterization of Heterocyclic Compounds
- Insect and Pesticide Research
- Echinoderm biology and ecology
- Cholinesterase and Neurodegenerative Diseases
- Inorganic and Organometallic Chemistry
- Insect Pest Control Strategies
- Carbohydrate Chemistry and Synthesis
- Marine and coastal plant biology
- Statistical Methods in Clinical Trials
- Fern and Epiphyte Biology
- Polyamine Metabolism and Applications
- Phytochemical compounds biological activities
- Natural Compound Pharmacology Studies
- Multicomponent Synthesis of Heterocycles
- Marine Sponges and Natural Products
University of the Basque Country
2023
Universidad de la República
2011-2022
Hospital Alemán
2019
Universidade Estadual Paulista (Unesp)
2011
Centro Uruguayo de Imagenología Molecular
1998-2010
Instituto de Botânica
2001-2006
Universidad de Montevideo
1998
Eleven sesquiterpenes (1−11) and one long chain aldehyde (12) have been isolated from the dichloromethane extract of red alga Laurencia scoparia. Four them are new natural products. Scopariol (1) is a product with an unusual rearranged chamigrane-type structure. The other three β-chamigrenes: isorigidol (2), (+)-3-(Z)-bromomethylidene-10β-bromo-β-chamigrene (3), (−)-3-(E)-bromomethylidene-10β-bromo-β-chamigrene (4). in vitro activity compounds 1−12 against parasitant stage Nippostrongylus...
Chondriamide C (3), a new bis(indole) amide, was isolated from the red alga Chondria atropurpurea, and its structure established spectroscopic data chemical transformations. A natural product, 3-indoleacrylamide (4), previously described chondriamides B (1, 2) 3-indoleacrylic acid (5) were also isolated. The anthelmintic activities of compounds 1, 3, 4, 6 (the O,N1,N1'-trimethyl derivative compound against Nippostrongylus brasiliensis in vitro evaluated.
Three novel halogenated beta-bisabolene sesquiterpenoids (1-3), together with two know triquinane alcohol sesquiterpenes (6 and 7), were isolated from the red alga Laurencia scoparia their structures elucidated by spectroscopic methods. Single-crystal X-ray crystallography allowed us to confirm structure of 1 as well determine absolute configuration all stereocenters. To best our knowledge, isolation beta-bisabolenes genus has no precedent in literature. Compound showed weak vitro...
Abstract Background Helminthiasis and resistance to commercial anthelmintic compounds are major causes of economic losses for livestock producers, resulting in an urgent need new drugs reliable vitro screening tests capable detecting potentially active products. Considering this, a series novel benzimidazole derivatives (5-methylbenzimidazole 1,2-disubstituted, 5-carboxybenzimidazole, 5-methylbenzimidazole 2-one) was screened on exsheathed L3 (xL3) the adult stage Haemonchus contortus (Kirby...
Some novel valerolactam derivatives of 5(6)-substituted-(1H-benzimidazol-2-yl-amine) were constructed based on the union two structural domains with anthelmintic activity. The tested hybrid compounds 7-9 exhibited greater activity using Nippostrongylus brasiliensis physiology-based in vitro bioassay comparison to commercial benzimidazoles. Moreover, improved physicochemical properties compared domain allowed penetration parasite barriers, concurrently an increased intraparasitary...
Abstract The effect of praziquantel (PZQ) on the strobilar development cyclophyllidean cestode Mesocestoides corti was explored. larvae were cultivated under conditions reported to favour their differentiation adult stage. Parasites exposed 0.1 μg ml -1 PZQ for 16 h and subsequently transferred drug-free medium. ocurrence segmentation — an early event larval somatic worm considered as quantitative data. This phenomenon evidenced earlier in worms transiently with respect control cultures....
The nematocidal in vitro activity of three natural perrottetins (phenolic bisbibenz-ylethers) and eleven diphenyl ethers used as synthetic precursors has been assayed using two different experimental models, <i>Caenorhabditis elegans</i> <i>Nippostrongylus brasiliensis.</i> Nine compounds showed some against C. <i>elegans</i> nine N. <i>brasiliensis.</i> For the former model, displayed an similar to that standards, whereas for <i>brasiliensis</i> none tested was active standards. From <i>in...
Abstract Several new pyrazolo[1,5‐ a ]pyrimidines were obtained from the reaction of 1 H ‐5‐amino‐3‐phenylpyrazole ( ) with β‐dimethylaminopropiophenones 2 in pyridine. The structure elucidation 6,7‐dihydropyrazolo[1,5‐ 3 is based on nmr measurements. These compounds showed moderate anthelmintic vitro activity against Nipposirongylus brasiliensis model.
In the search for acetylcholinesterase inhibitors as a potential target discovery of anthelmintic drugs, series 27 pyridinic and pyrazinic compounds have been designed on basis molecular hybridization two known AChE inhibitors, namely, tacrine (-)-3-O-acetylspectaline, concept isosterism. The synthesized generally presented moderate anticholinesterasic activities when compared with positive control physostigmine, but one compound (ethyl 2-[(6-chloropyrazin-2-yl)sulfanyl] acetate) exhibited...
Using different heterocycle formation methodologies (Deoxo-Fluor, DAST, POCl3, TosMIC), [2,5]bis-1,3- azoles were prepared as stable analogs of bengazoles, a family potent anthelmintic marine natural products. The cytotoxic activity these heterocycles and their precursors on HCT-15 cells the effect L4 larvae Nippostrongylus brasiliensis evaluated. Keywords: Bis-1, 3-azoles, Anthelmintic, Cytotoxic, Bengazoles
Tandem cyclizations to [2,5] bis-1,3-azoles provided simplified and stable models of biological active marine natural products. The cytotoxic activity in HCT-15 cells the effect on L4 larvae Nippostrongylus brasiliensis heterocycles were evaluated data that serve for preparation bioselective new therapeutic agents. Keywords: Bis-1,3-azoles, anthelmintic, cytotoxic, Bengazoles
Aim: Understanding a drug dissolution process from solid dispersions (SD) to develop formulations with predictable in vivo performance. Materials & methods: Dissolution data of fenbendazole released the SDs and control physical mixtures were analyzed using Lumped mathematical model estimate parameters pharmaceutical relevance. Results: The fit obtained by showed that all have unique profile an error ±4.1% initial release rate 500-times higher than pure drug, without incidence drug/polymer...