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Lancelot JC, Robba M, Bonnet JJ, Vaugeois JM, Costentin J. 
“Synthesis and preliminary study of the activity of thiophene analogues of pyrovalerone on the neuronal uptake of the monoamines”. 
Eur J Med Chem. 1992;27:297-300.

Application of the concept of benzene-thiophene isosterism to structural changes led to an improvement in the pharmaceutical profile of certain compounds [l-6]. We have used this previously in the area of spasmolytic or peripheral vasodilator activities with P-substituted thiophene derivatives [7-91. In the context of the investigation of substances with a psychostimulant activity, and using the model of 2-Npyrrolidino- 1 -p-tolyl- 1 -pentanone (pyrovalerone) 1 [lO-141, we chose substitution of thiophene in 2 position and studied a series of 2 amino-1-(2-thienyl)-lpentanones.

These aminoketones were evaluated in comparison with pyrovalerone 1 with regard to their inhibition of the monoamines (dopamine, norepinephrine, serotonine) uptake and to the dopamine release by synaptosomal preparations of rat brain.
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