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2-Aryladenine derivatives as a potent scaffold for adenosine receptor antagonis...

Areias, Filipe; Correia, Carla; Rocha, Ashly; Teixeira, Sofia; Castro, Marián; Brea, Jose; Hu, Huabin; Carlsson, Jens; Loza, Maria I.

A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A<inf>1</inf>, A<inf>2A</inf>, A<inf>2B</inf>, and A<inf>3</inf> adenosine receptor subtypes. Eleven purines showed potent antagonism at A<inf>1</inf>, A<inf>3</inf>, dual A<inf>1</inf>/A<inf>2A</inf>, A<inf>1</inf>/A<inf>2B</inf>, or A<inf>1</inf>/A<inf>3</inf> adenosine receptor...


2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenos...

Areias, Filipe; Correia, Carla; Rocha, Ashly; Brea, José; Castro, Marián; Loza, Maria I.; Proença, M. Fernanda R. P.; Carvalho, M. Alice

From a collection containing more than 1500 academic compounds, in silico screening identified a hit for the human A1 adenosine receptor containing a new purine scaffold. To study the structure activity relationships of this new chemical series for adenosine receptors, a library of 24 purines was synthesized and tested in radioligand binding assays at human A1, A2A, A2B and A3 adenosine receptor subtypes. Fourt...


New nitrogen compounds coupled to phenolic units with antioxidant and antifunga...

Bettencourt, Ana Paula; Castro, Marián; Silva, João; Fernandes, Francisco; Coutinho, O. P.; Sousa, Maria João; Proença, M. Fernanda R. P.

A selection of 1-amino-2-arylidenamine-1,2-(dicyano)ethenes <b>3</b> was synthesized and cyclized to 2-aryl-4,5-dicyano-1<i>H</i>-imidazoles <b>4</b> upon reflux in ethyl acetate/acetonitrile, in the presence of manganese dioxide. These compounds were tested for their antioxidant capacity by cyclic voltammetry, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and deoxyribose degradation assays. The minimum inhibito...


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