Browsing by Author "Silva, Vera L.M."
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- Arylxanthones and arylacridones: a synthetic overviewPublication . Santos, Clementina M.M.; Pinto, Diana; Silva, Vera L.M.; Silva, ArturArylxanthones and arylacridones although not yet found in nature are becoming an important group of heterocyclic compounds due to their promising biological activities. Their central cores, xanthone and acridone, are recognized as interesting motifs for drug development mainly to be used in antitumour chemotherapy. The synthesis of this type of compounds is still scarce but several successful examples were recently published and a large variety of arylated xanthone and acridone derivatives were prepared. A systematic survey of the literature dedicated to their synthesis will be presented and discussed in this review.
- Quinolinones and related systems (Update 2022)Publication . Silva, Vera L.M.; Pinto, Diana; Santos, Clementina M.M.; Rocha, DjenisaQuinolinones, of which the quinolin-4(1H)-one ring system can be highlighted, represent an exciting class of nitrogen heterocycles. The quinolinone motif can be found in many natural compounds and approved drugs for several diseases. This chapter is a comprehensive survey of the methods for the synthesis of quinolin-2(1H)-ones, quinolin-4(1H)-ones, and their thio- and amino derivatives, and is an update to the previous Science of Synthesis chapter (Section 15.4), covering the period between 2003 and 2020.
- A study towards drug discovery for the management of type 2 diabetes: Mellitus through inhibition of the carbohydrate-hydrolyzing enzymes α-amylase and α-glucosidase by chalcone derivativesPublication . Rocha, Sónia; Sousa, Adelaide; Ribeiro, Daniela; Correia, Catarina M.; Silva, Vera L.M.; Santos, Clementina; Silva, Artur; Araújo, Alberto N.; Fernandes, Eduarda; Freitas, MarisaThe inhibition of carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, is one of the major therapeutic strategies for the treatment of type 2 diabetes mellitus. Chalcones have been recognized for their multiple biological activities, including antidiabetic properties, through unclear mechanisms. In the present work, a panel of chalcones bearing hydroxy, methoxy, methyl, nitro, chloro, fluoro and bromo substituents were evaluated against α-amylase and α-glucosidase activities, most of them for the first time. The results showed that the substitution patterns and the type of substituents of chalcones influence their inhibitory activity. The presence of hydroxy groups at C-2’- and C-4’ of the A ring and at C-3 and C-4 of the B ring favors the intended effect. Chalcones holding nitro groups and chloro substituents, together with a hydroxy group in the chalcone scaffold, showed strong inhibition of the α-glucosidase activity. The present study provides related scaffolds that may serve as the basis for the design and synthesis of new structures in order to obtain the ideal antidiabetic chalcone.
- Synthesis of chromone-related pyrazole compoundsPublication . Santos, Clementina M.M.; Silva, Vera L.M.; Silva, ArturChromones, six-membered oxygen heterocycles, and pyrazoles, five-membered two-adjacent-nitrogen-containing heterocycles, represent two important classes of biologically active compounds. Certain derivatives of these scaffolds play an important role in medicinal chemistry and have been extensively used as versatile building blocks in organic synthesis. In this context, we will discuss the most relevant advances on the chemistry that involves both chromone and pyrazole rings. The methods reviewed include the synthesis of chromone-pyrazole dyads, synthesis of chromone-pyrazole-fused compounds, and chromones as starting materials in the synthesis of 3(5)-(2-hydroxyaryl)pyrazoles, among others. This review will cover the literature on the chromone and pyrazole dual chemistry and their outcomes in the 21st century.