Microwave-assisted synthesis of thieno[2,3-c]pyridine derivatives as a new series of allosteric enhancers at the adenosine A(1) receptor

The microwave-assisted aromatization method has been used for the synthesis of a series of novel thieno[2,3-c]pyridines. This rapid method produces compounds in good yield within minutes in comparison with conventional heating method. The synthesized molecules have been evaluated as a potential new...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-11, Vol.16 (21), p.5530-5533
Main Authors: Romagnoli, Romeo, Baraldi, Pier Giovanni, Moorman, Allan R, Iaconinoto, Maria Antonietta, Carrion, Maria Dora, Cara, Carlota Lopez, Tabrizi, Mojgan Aghazadeh, Preti, Delia, Fruttarolo, Francesca, Baker, Stephen P, Varani, Katia, Borea, Pier Andrea
Format: Article
Language:English
Subjects:
Allosteric Regulation - physiology
Microwaves
Pyridines - chemical synthesis
Pyridines - pharmacology
Receptor, Adenosine A1 - metabolism
Thiophenes - chemical synthesis
Thiophenes - pharmacology
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Summary:The microwave-assisted aromatization method has been used for the synthesis of a series of novel thieno[2,3-c]pyridines. This rapid method produces compounds in good yield within minutes in comparison with conventional heating method. The synthesized molecules have been evaluated as a potential new series of allosteric enhancers acting at the adenosine A(1) receptor. In a functional assay, one compound (3h) showed activity comparable with that of reference compound PD 81,723.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2006.08.041