A5064488322- Synthesis and Biological Evaluation
- Synthesis and biological activity
- Synthesis of Organic Compounds
- Cholinesterase and Neurodegenerative Diseases
- Click Chemistry and Applications
- Computational Drug Discovery Methods
- Free Radicals and Antioxidants
- Adenosine and Purinergic Signaling
- Electrochemical sensors and biosensors
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Phytochemicals and Antioxidant Activities
- melanin and skin pigmentation
- Bioactive Compounds and Antitumor Agents
- Chronic Obstructive Pulmonary Disease (COPD) Research
- Chemical Synthesis and Analysis
- Monoclonal and Polyclonal Antibodies Research
- Chemical synthesis and alkaloids
- Asthma and respiratory diseases
- Synthesis and Reactions of Organic Compounds
- Parkinson's Disease Mechanisms and Treatments
- Plant chemical constituents analysis
- Oxidative Organic Chemistry Reactions
- Receptor Mechanisms and Signaling
- Trypanosoma species research and implications
Universidade de Santiago de Compostela
2016-2025
Universidade do Porto
2014-2023
Center for Research in Molecular Medicine and Chronic Diseases
2023
University of Cambridge
2016-2022
University of Coimbra
1996-2022
Instituto Português de Oncologia Francisco Gentil
2020
Hospitais da Universidade de Coimbra
2005-2017
Rede de Química e Tecnologia
2016
Faculdade de Tecnologia e Ciências
2016
Administração Regional de Saúde de Lisboa e Vale do Tejo
2016
Site-selective chemical conjugation of synthetic molecules to proteins expands their functional and therapeutic capacity. Current protein modification methods, based on biochemical technologies, can achieve site selectivity, but these techniques often require extensive sequence engineering or are restricted the N- C-terminus. Here we show computer-assisted design sulfonyl acrylate reagents for a single lysine residue native sequences. This feature designed acrylates, together with innate...
Abstract Maleimides remain the reagents of choice for preparation therapeutic and imaging protein conjugates despite known instability resulting products that undergo thiol-exchange reactions in vivo . Here we present rational design carbonylacrylic chemoselective cysteine bioconjugation. These rapid thiol Michael-addition under biocompatible conditions stoichiometric amounts. When using equipped with PEG or fluorophore moieties, this method enables access to antibody precisely modified at...
New series of 6-substituted-3-arylcoumarins displaying several alkyl, hydroxyl, halogen, and alkoxy groups in the two benzene rings have been designed, synthesized, evaluated vitro as human monoamine oxidase A B (hMAO-A hMAO-B) inhibitors. Most studied compounds showed a high affinity selectivity to hMAO-B isoenzyme, with IC50 values on nanomolar picomolar range. Ten 22 described displayed higher MAO-B inhibitory activity than selegiline. Coumarin 7 is most active compound this series, being...
Antibiotic resistance is one of the main public health concerns this century. This also associated with oxidative stress, which could contribute to selection resistant bacterial strains. Bearing in mind, and considering that flavonoid compounds are well known for displaying both activities, we investigated a series hydroxy-3-arylcoumarins structural features flavonoids their antibacterial activity against different Active showed selectivity studied Gram-positive bacteria compared...
Abstract Alzheimer’s disease (AD) is a neurodegenerative disorder representing the leading cause of dementia and affecting nearly 44 million people worldwide. AD characterized by progressive decline in acetylcholine levels cholinergic systems, which results severe memory loss cognitive impairments. Expression activity butyrylcholinesterase (BChE) enzyme has been noted to increase significantly late stages AD, thus making it viable drug target. A series hydroxylated 2-phenylbenzofurans...
Chemical modification of proteins is essential for a variety important diagnostic and therapeutic applications. Many strategies developed to date lack chemo- regioselectivity as well result in non-native linkages that may suffer from instability vivo adversely affect the protein's structure function. We describe here reaction N-nucleophiles with amino acid dehydroalanine (Dha) protein context. When Dha chemically installed proteins, addition wide-range enables rapid formation amine...
The complex etiology of Alzheimer's disease (AD) has encouraged active research in the development multi-target drugs with two or more complementary biological activities, since they may represent an important advance treatment this disease. A series 3-substituted coumarins were synthesized and evaluated as monoamino oxidases (MAO) acetylcholinesterase (AChE) inhibitors. Most 3-benzamide coumarin derivatives inhibited both MAO-B AChE values micromolar range. It might be a promising direction...
A series of novel hydroxy-coumarin-chalcone hybrid compounds 2a-i has been synthesized by employing a simple and efficient methodology. An electrochemical characterization using cyclic voltammetry ESR spectroscopy were carried out to characterize the oxidation mechanism for target compounds. The antioxidant capacity reactivity determined ORAC assays, respectively. Biological assays assessed evaluate cytotoxicity cytoprotection against ROS/RNS on BAEC. results revealed that all tested present...
We describe the development of a bifunctional linker that simultaneously allows site-specific protein modification and palladium-mediated bioorthogonal decaging.
A new series of amino/nitro-substituted 3-arylcoumarins were synthesized and their antibacterial activity against clinical isolates Staphylococcus aureus (Gram-positive) Escherichia coli (Gram-negative) was evaluated. Some these molecules exhibited S. comparable to the standards used (oxolinic acid ampicillin). The preliminary structure-activity relationship (SAR) study showed that depends on position 3-arylcoumarin substitution pattern. With aim finding structural features for selectivity,...
Abstract Quaternized vinyl‐ and alkynyl‐pyridine reagents were shown to react in an ultrafast selective manner with several cysteine‐tagged proteins at near‐stoichiometric quantities. We have demonstrated that this method can effectively create a homogenous antibody–drug conjugate features precise drug‐to‐antibody ratio of 2, which was stable human plasma retained its specificity towards Her2+ cells. Finally, the developed warhead introduces +1 charge overall net protein, enabled us show...
In the present work we report on contribution of coumarin moiety to tyrosinase inhibition. Coumarin-resveratrol hybrids 1-8 have been resynthesized investigate structure-activity relationships and IC(50) values these compounds were measured. The results showed that exhibited inhibitory activity. Compound 3-(3',4',5'-trihydroxyphenyl)-6,8-dihydroxycoumarin (8)is most potentcompound (0.27 mM), more so than umbelliferone (0.42 used as reference compound. kinetic studies revealed compound 8...
Based on the observed biological activities of coumarins and chalcones, we have synthesized coumarin–chalcone hybrids with aim evaluating their antioxidant properties trypanocidal activity against Trypanosoma cruzi, parasite responsible for Chagas disease. All derivatives been proved to be good antioxidants in spite moderate epimastigote stage (clone Dm28c). these results, can conclude that compounds 4 5 are potential candidates vitro studies activity. These preliminary findings encourage us...
The dramatic worldwide increase of dangerous infections by resistant and multi-resistant microbes makes the search new molecules chemical entities an important topic in Medicinal Chemistry. As ideal drug candidate has not been attained, intensive for innovative antimicrobials is still needed. A small series 3- amino/nitrocoumarins without substitutions or substituted methyl methoxy groups at different positions were synthesized evaluated their antibacterial antifungal activities against...