14 documents found, page 1 of 2

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Pyrazoles as potential modulators of inflammation through the inhibition of COX...

Silva, Jorge; Rocha, Sónia; Silva, Vera L. M.; Silva, Artur M. S.; Moreira, Fernando; Fernandes, Eduarda; Freitas, Marisa

The inflammatory process is a complex and tightly regulated cascade of events that involves the production of prostaglandins (PG) by the inducible isoform cyclooxygenase 2 (COX-2) and the production of reactive pro-oxidant species. When the production of these mediators becomes excessive, it can lead to chronic inflammation and associated diseases such as diabetes, rheumatoid arthritis, and cancer. Unfortunatel...


Facile Access to Structurally Diverse Antimalarial Indoles Using a One-Pot A3 C...

da Silva, Gustavo; Luz, André F. S.; Duarte, Denise; Fontinha, Diana; Silva, Vera L. M.; Almeida Paz, Filipe A.; Madureira, Ana M.; Simões, Sandra

A multistep and diversity-oriented synthetic route aiming at the A3 coupling/domino cyclization of o-ethynyl anilines, aldehydes and s-amines is described. The preparation of the corresponding precursors included a series of transformations, such as haloperoxidation and Sonogashira cross-coupling reactions, amine protection, desilylation and amine reduction. Some products of the multicomponent reaction underwen...


Facile access to structurally diverse antimalarial indoles using a one‐pot A3 c...

Silva, Gustavo Da; Luz, André F. S.; Duarte, Denise; Fontinha, Diana; Silva, Vera L. M.; Almeida Paz, Filipe A.; Madureira, Ana Margarida

A multistep and diversity-oriented synthetic route aiming at the A3 coupling/domino cyclization of o-ethynyl anilines, aldehydes and s-amines is described. The preparation of the corresponding precursors included a series of transformations, such as haloperoxidation and Sonogashira cross-coupling reactions, amine protection, desilylation and amine reduction. Some products of the multicomponent reaction underwen...


An in silico and an in vitro inhibition analysis of glycogen phosphorylase by f...

Rocha, Sónia; Aniceto, Natália; Guedes, Rita C.; Albuquerque, Hélio M. T.; Silva, Vera L. M.; Silva, Artur M. S.; Corvo, Maria Luísa; Fernandes, Eduarda

Glycogen phosphorylase (GP) is a key enzyme in the glycogenolysis pathway. GP inhibitors are currently under investigation as a new liver-targeted approach to managing type 2 diabetes mellitus (DM). The aim of the present study was to evaluate the inhibitory activity of a panel of 52 structurally related chromone derivatives; namely, flavonoids, 2-styrylchromones, 2-styrylchromone-related derivatives [2-(4-aryl...


Customizable and Regioselective One-Pot N−H Functionalization of DNA Nucleobase...

Rocha, Djenisa H. A; Machado, Carmen M.; Sousa, Vera; Sousa, Cristiana F. V.; Silva, Vera L. M.; Silva, Artur M.; Borges, João; Mano, João F.

DNA is one of the most exciting biomolecules in nature for developing supramolecular biofunctional nanoarchitectures owing to the highly specific and selective interactions between complementary Watson-Crick base pairing. Herein, simple and one-pot synthetic procedures have been implemented for producing a library of DNA nucleobase derivatives endowed with reactive functional groups for bioconjugation and cross...


“Só para ensinar” ou “mais para aprender”? Reflexões, entre pares, sobre as (pr...

Franco, Amanda; Vieira, Rui Marques; Simões, Ana Raquel; Costa, Alberto J.; Ventura, Sónia P. M.; Neto, Vitor; Carlos, Vânia; Lopes, Betina Silva

Várias estratégias têm sido avançadas para suprir lacunas na formação pedagógica de professores do Ensino Superior, sendo uma delas a observação por pares. Com o intuito de apoiar os professores nas suas práticas pedagógicas, está em curso na Universidade de Aveiro (Portugal) um programa de observação por pares, já na sua segunda edição. No presente artigo, após um breve enquadramento aludindo à profissionalida...


Is it “just to teach” or is it “more to learn”? Reflections, among peers, about...

Franco, Amanda; Vieira, Rui Marques; Simões, Ana Raquel; Costa, Alberto; Ventura, Sónia P. M.; Neto, Victor; Carlos, Vânia; Lopes, Betina Silva

Several strategies have been proposed to fill the gaps in the pedagogical training of faculty, one of which referring to peer observation of teaching. To support faculty in their pedagogical practices, a peer observation of teaching program is currently being implemented at University of Aveiro (Portugal), already in its second edition. In the present paper, after briefly framing the concept of teaching profess...

Date: 2020   |   Origin: Indagatio Didactica

Current progress on antioxidants incorporating the pyrazole core

Silva, Vera L. M.; Elguero, J.; Silva, Artur M. S.

The search of new antioxidants, as drugs candidates, is an active field of medicinal chemistry. The synthesis of compounds with antioxidant potential has increased in recent years and a high number of structurally diverse compounds have been published. This review aims to show the current state-of-the-art on the development of antioxidant compounds incorporating the pyrazole pharmacophore. It is a well-timed re...


Synthesis of 3-(2-nitrovinyl)-4H-chromones: useful scaffolds for the constructi...

Soengas, Raquel G.; Silva, Vera L. M.; Ide, Daisuke; Kato, Atsushi; Cardoso, Susana M.; Almeida Paz, Filipe A.; Silva, Artur M. S.

The Henry-type Barbier addition of bromonitromethane to 3-formylchromone, immediately followed by acetylation and concomitant elimination to afford nitroalkenes in excellent yield and total (E)-selectivity is described. Cycloaddition of N-methylhydrazones with the obtained nitroalkenes gave the corresponding pyrazoles. Among the prepared pyrazoles, derivative 6j, which contains a catechol moiety, showed simulta...


Synthesis, Post-Modification and Fluorescence Properties of Boron Diketonate Co...

Guieu, Samuel; Pinto, Joana; Silva, Vera L. M.; Rocha, João; Silva, Artur M. S.

A family of fluorescent dyes based on a boron diketonate core with extended conjugation has been prepared by a three‐step strategy. The complexes are fluorescent both in solution and in the solid state,...


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