2-Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers

Abstract Three series of 2-amino-4,5,6,7-tetrahydrobenzo[ b ]thiophene and 2-amino-5,6,7,8-tetrahydrocyclohepta[ b ]thiophenes with 3-carboxylates and carboxamides have been prepared using the Gewald synthesis and evaluated as A 1 AR allosteric enhancers. The structure–activity relationships of these classes of compound are described. A number of compounds, notably 7b , are more potent and efficacious than PD81,723 ( 1 ).