Bioorganic & Medicinal Chemistry Letters 2006-11-01

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

Romeo Romagnoli, Pier Giovanni Baraldi, Allan R Moorman, Maria Antonietta Iaconinoto, Maria Dora Carrion, Carlota Lopez Cara, Mojgan Aghazadeh Tabrizi, Delia Preti, Francesca Fruttarolo, Stephen P Baker, Katia Varani, Pier Andrea Borea

Index: Bioorg. Med. Chem. Lett. 16(21) , 5530-3, (2006)

Full Text: HTML

Abstract

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.