2-Aminothiophene-3-carboxylates and carboxamides as adenosine A 1 receptor allosteric enhancers

G Nikolakopoulos, H Figler, J Linden…

Index: Nikolakopoulos, George; Figler, Heidi; Linden, Joel; Scammells, Peter J. Bioorganic and Medicinal Chemistry, 2006 ,  vol. 14,  # 7  p. 2358 - 2365

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Citation Number: 84

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 A1AR 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).