A5017415635- Research on Leishmaniasis Studies
- Computational Drug Discovery Methods
- Trypanosoma species research and implications
- Cancer therapeutics and mechanisms
- Piperaceae Chemical and Biological Studies
- Synthesis and biological activity
- Multicomponent Synthesis of Heterocycles
- Synthesis and bioactivity of alkaloids
- Synthesis and Reactivity of Heterocycles
- Bioactive Compounds and Antitumor Agents
- Synthesis and Biological Evaluation
- Enzyme function and inhibition
- Rural Development and Agriculture
- Parasites and Host Interactions
- Hemoglobin structure and function
- Malaria Research and Control
- Cholesterol and Lipid Metabolism
- Marine Sponges and Natural Products
- Protein Structure and Dynamics
- Microwave-Assisted Synthesis and Applications
- Cancer Treatment and Pharmacology
- Lipid metabolism and disorders
- Antioxidant Activity and Oxidative Stress
- Phytochemistry and biological activities of Ficus species
- Cellular Mechanics and Interactions
Universidade Estadual de Campinas (UNICAMP)
2021-2025
University of Vassouras
2024
Instituto de Tecnología Química
2022
Universidade Federal da Paraíba
2011-2019
Universidade Federal do Rio de Janeiro
1988-2018
Chagas disease (CD), caused by the flagellate protozoan Trypanosoma cruzi, is a neglected tropical endemic in 21 countries. The only two antiparasitic drugs approved for its treatment, benznidazole and nifurtimox, have significant drawbacks. We present herein optimization of series substituted indoles that were identified through phenotypic screening against T. cruzi. Early lead compounds with balanced potency physicochemical properties advanced to animal studies but showed limited plasma...
Tumor aggressiveness is usually associated with metastasis. MDA-MB 231, a triple-negative breast cancer (TNBC), an aggressive type of and early The Rho/ROCK pathway key regulator cell motility involving cytoskeleton regulation through stabilization actin filaments stress fiber formation. In this study we show that Fasudil, ROCK inhibitor, inhibited the migration 231 A549 cells, without altering viability these cells at concentration 10 μM, modified tumor morphology, disorganization fibers...
Leishmaniasis represents a series of severe neglected tropical diseases caused by protozoa the genus Leishmania and is widely distributed around world. Here, we present syntheses Morita-Baylis-Hillman adducts (MBHAs) prepared from eugenol, thymol carvacrol, their bioevaluation against promastigotes amazonensis. The new MBHAs are in two steps essential oils moderate to good yields IC50 values range 22.30-4.71 μM. Moreover, selectivity index most potent compound very high (SIrb > 84.92), far...
It is reported the synthesis of 24 Morita-Baylis-Hillman adducts (3a-3l/6a-6l) using microwave irradiation at 80 ºC or conventional protocol 0 to promote reactions between aromatic aldehydes and methyl acrylate acrylonitrile (81-99%). shown that reaction 2-hydroxy(4-bromophenyl)methyl formation reversible 120 ºC.
Piperin is the active compound of black pepper (Piper nigrum). From piperine was obtained molecule piperic acid (PAC). The objective this study to evaluate antinociceptive and anti-inflammatory compound. effects PAC were evaluated by abdominal writhing, formalin, capsaicin tail-flick tests; while paw oedema air pouch tests, in vitro COX inhibition assay. possible action mechanism using naloxone, L-NAME, glibenclamide atropine tail flick test Cholinesterase activity assay production TNF-α...
In this work, a microwave-assisted synthesis study by microwave irradiation to produce indolizine-2-carbonitrile and indolizine-2-carboxylate in good high yields (70 81%, respectively) one step from Morita-Baylis-Hillman adducts (MBHA) is presented. These compounds were subsequently transformed (94 100%, three 2-indolizine derivatives. The five synthesized designed silico aiming present potential selective activities as ion channel modulators. suggested the score values using Molinspiration...
In this study, we synthesized a new congener series of N-sulphonylhydrazones designed as candidate ROCK inhibitors using the molecular hybridization clinically approved drug fasudil (1) and IKK-β inhibitor LASSBio-1524 (2). Among compounds, N-methylated derivative 11 (LASSBio-2065) showed best inhibitory profile for both isoforms, with IC50 values 3.1 3.8 µM ROCK1 ROCK2, respectively. Moreover, these compounds were also active in scratch assay performed human breast cancer MDA-MB 231 cells...
Neste artigo, um estudo sintético assistido por irradiação de micro-ondas para produzir 2-indolizina-carbonitrila e 2-indolizina-carboxilato metila em bons a altos rendimentos (70 81%) uma etapa partir adutos Morita-Baylis-Hillman (AMBH) é apresentado.Estes compostos foram subsequentemente transformados (94-100%) três derivados 2-indolizínicos.Os cinco sintetizados idealizados in silico objetivando potenciais atividades seletivas como moduladores canais iônicos.Estas sugeridas pelos valores...
Piperine is the major alkaloid of Piper nigrum Linn., used as a spice and in folk medicine.We present molecular docking study supporting experimental data on enhancement bioavailability propranolol, theophylline, phenytoin, nevirapine, nimesulide, pyrazinamide, carbamazepine, spartein presence piperine.The complex formed with piperine CYP3A4 was shown to be most stable all, binding energy -8.60 kcal/mol.This explains related mechanism drug-herb interaction, since better anchoring active site...
Chagas disease (CD) is a parasitic neglected tropical (NTD) caused by the protozoan
A pesquisa bibliográfica apresentada por meio deste artigo acadêmico, tem como pano de fundo a descrição breve da história produção e distribuição eletricidade no Brasil, trás um resumo sobre operação serviços iniciados pelo grupo Light Amforp entre os anos 1880 1890. Aborda-se ainda meta estabelecida pela ONU através Agenda 2030, quanto transição para energia limpa acessível todos do ODS 7. E fim, destacamos fotovoltaica fonte energética impasses relacionados à plena expansão sua utilização...
Hypertension is one of the major risk factors associated with cardiovascular diseases, requiring discovery new pharmacologically active compounds.The versatility Morita-Baylis-Hillman (AMBH) adducts from perspective medicinal chemistry has been placing this class polyfunctional molecules in evidence recent years due their expressive biological activities.Therefore, work describes an exploratory study potential vasorrelaxant activity AMBH derived eugenol.These compounds were tested by...
The ATP analog arylazido-ATP 5'-triphosphate) (3'-O-(3-[N-(4-azido-2-nitrophenyl)amino]propionyl)adenosine was shown to phosphorylate the calcium-ATPase from sarcoplasmic reticulum in absence of calcium. Levels 0.6 nmol phosphoenzyme/mg protein were attained. Calcium either at micromolar or millimolar concentrations did not affect level phosphoenzyme. A non-Michaelian dependence hydrolytic activity as a function concentration obtained addition modify for activation hydrolysis maximal rate...
The ability of cancer cells to undergo invasion and migration is a prerequisite for tumor metastasis. Rho, Ras-related small GTPase, the Rho-associated coiled coil–containing protein kinases (Rho kinases, ROCK1 ROCK2), are key regulators focal adhesion, actomyosin contraction, thus cell motility. concept Rho Kinase inhibition as an antimetastatic therapy can now be clinically explored. Therefore, it great interest investigate whether Fasudil kinase inhibitor) affects early events in human...
Many patients with metastatic tumors have substantially worse survival in comparison those nonmetastatic tumors. The ability of cancer cells to undergo invasion and migration is a prerequisite for tumor metastasis these events became targets the development new antimetastatic drugs. Rho kinases, ROCK1 ROCK2, are key regulators focal adhesion, actomyosin contraction, thus cell motility. In this regard our group synthesized two sulfonylhydrazones, analogous Fasudil (a classic kinase...
ARTEMISININ AND DERIVATIVES: DISCOVERY, SYNTHETIC STRATEGIES, INDUSTRIAL PRODUCTION. Artemisinin, a natural sesquiterpene isolated from the Artemisia annua L. plant, represents remarkable achievement in treatment against malaria. Since its discovery 1970’s, researchers readily started synthesizing this complex product containing an unusual endoperoxide fragment. Despite various total syntheses reported, only last decade production jumped extraction/bench scale to industrial manufacturing. In...