Romagnoli R1, Baraldi PG2, Carrion MD3, Cruz-Lopez O3, Cara CL3, Saponaro G3, Preti D3, Tabrizi MA3, Baraldi S3, Moorman AR4, Vincenzi F5, Borea PA5, Varani K5.
Bioorg Med Chem. 2014 Jan 1;22(1):148-66. doi: 10.1016/j.bmc.2013.11.043. Epub 2013 Dec 1.2-Amino-3-benzoyl thiophenes have been widely reported to act as allosteric enhancers at the A1 adenosine receptor. Their activity can be increased considerably by appropriate substitutions at the 4- and 5-positions of the thiophene ring. Substituent size at the thiophene C-4 position seemed to be a factor closely related to activity, with the 4-neopentyl (2,2-dimethylpropyl) substitution showing the greatest enhanced activity. Read More